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Imatinib (STI571) Mesylate Inibitore della Tirosin Chinasi
N. Cat.S1026
Struttura chimica
Peso molecolare: 589.71
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Coltura cellulare, trattamento e concentrazione di lavoro
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | PMID |
|---|---|---|---|---|---|---|
| GIST882 | Growth Inhibition Assay | 96 h | IC50=1.7 μM | 24900212 | ||
| K562 | Cytotoxicity Assay | 24 h | IC50=0.21 μM | 22000207 | ||
| MCF-7 | Cytotoxicity Assay | 24 h | IC50=0.83 μM | 22000207 | ||
| MDA-MB-23 | Cytotoxicity Assay | 24 h | IC50=1.8 μM | 22000207 | ||
| K562r | Growth Inhibition Assay | IC50=10 μM | 24939418 | |||
| K562 | Growth Inhibition Assay | EC50=0.09 μM | 16678414 | |||
| MCF-7 | Growth Inhibition Assay | 10 μM | 48 h | blocks cell proliferation increase induced by BJ3Z | 25274034 | |
| K-562 | Growth Inhibition Assay | IC50=1 μM | 25239662 | |||
| K562 | Growth Inhibition Assay | IC50=0.5 μM | 24939418 | |||
| PC3 | Apoptosis Assay | 20 μM | 48/72 h | increases cell survival | 25786656 | |
| PC3 | Cell Viability Assay | 20 μM | 6-72 h | increases cell viability | 25786656 | |
| DU145 | Apoptosis Assay | 20 μM | 48/72 h | induces cell death by apoptosis | 25786656 | |
| DU145 | Cell Viability Assay | 20 μM | 6-72 h | decreases cell viability | 25786656 | |
| Hep G2 | Growth Inhibition Assay | IC50=31 μM | 25863232 | |||
| T47D | Growth Inhibition Assay | IC50=50 μM | 25863232 | |||
| EOL-1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 0.0002 μM. | 19301902 | ||
| EOL-1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human EOL-1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.001 μM. | 29544149 | ||
| GISTT1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.003 μM. | 28541695 | ||
| Sf9 | Function assay | Binding affinity to human active site of N-terminal hexahistidine-tagged ABL2 expressed in Trichoplusia ni infected Sf9 cells by isothermal titration calorimetric assay, Kd = 0.006 μM. | 21417343 | |||
| K562 | Antiproliferative assay | Antiproliferative activity against human imatinib-resistant K562 cells, IC50 = 0.00605 μM. | 21376587 | |||
| GISTT1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.008 μM. | 27077705 | ||
| GISTT1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.008 μM. | 27966954 | ||
| GISTT1 | Function assay | 72 hrs | Inhibition of KIT in human GISTT1 cells assessed as growth inhibition after 72 hrs by SRB assay, GI50 = 0.01 μM. | 23773153 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused PDGFRalpha (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.0107 μM. | 28541695 | ||
| TF1 | Cytotoxicity assay | Cytotoxicity against human TF1 cells expressing c-KIT mutation assessed as cell viability, IC50 = 0.013 μM. | 22221201 | |||
| GIST882 | Antiproliferative assay | 72 hrs | Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.014 μM. | 27077705 | ||
| GIST882 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.014 μM. | 27966954 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.017 μM. | 30204441 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-fused PDGFRbeta (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.019 μM. | 29544149 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused PDGFR-beta (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.019 μM. | 27966954 | ||
| GIST882 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GIST882 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.02 μM. | 28541695 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT C674S mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.0249 μM. | 28541695 | ||
| BA/F3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-PDGFRbeta kinase assessed as proliferation after 48 hrs by MTT assay, IC50 = 0.027 μM. | 16415863 | ||
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50 = 0.03 μM. | 26850004 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, EC50 = 0.034 μM. | 27010810 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-fused PDGFRalpha (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.034 μM. | 29544149 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused PDGFR-alpha (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.034 μM. | 27966954 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT V559D mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.036 μM. | 28541695 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells, IC50 = 0.039 μM. | 20817538 | |||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.039 μM. | 27077705 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused c-KIT V559D mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.039 μM. | 27966954 | ||
| MDCK2 | Function assay | 5 mins | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis, IC50 = 0.04 μM. | 23241029 | ||
| GISTT1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.04 μM. | 28991465 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA, IC50 = 0.043 μM. | 20817538 | |||
| K562 | Function assay | 30 mins | Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.043 μM. | 28280261 | ||
| MEG01 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MEG01 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.045 μM. | 28541695 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT L576P mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.0451 μM. | 28541695 | ||
| MO7e | Function assay | Inhibition of SCF-induced phosphorylation of c-Kit in MO7e cells by TR-FRET assay, IC50 = 0.046 μM. | 18447379 | |||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.046 μM. | 30204441 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 0.049 μM. | 19301902 | ||
| HEK293 | Function assay | 1.5 mins | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis, IC50 = 0.05 μM. | 23241029 | ||
| BA/F3 | Antiproliferative assay | 5 to 10 uM | 48 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Tel-SH2-KD assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50 = 0.055 μM. | 16415863 | |
| HT-29 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.06 μM. | 19469547 | ||
| K562 | Cytotoxicity assay | Cytotoxicity against human K562 cells assessed as reduction in cell viability, IC50 = 0.06 μM. | 26264503 | |||
| HT-29 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.06 μM. | 29724653 | ||
| JURL-MK1 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human JURL-MK1 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.06 μM. | 27011159 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.07 μM. | 30204441 | ||
| A31 | Function assay | Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA, IC50 = 0.072 μM. | 20817538 | |||
| A31 | Function assay | Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA, IC50 = 0.072 μM. | 20817538 | |||
| MEG01 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.074 μM. | 27077705 | ||
| MEG01 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.074 μM. | 27966954 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0771 μM. | 30137981 | ||
| BA/F3 | Antiproliferative assay | 5 to 10 uM | 48 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Tel-SH3-SH2-KD assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50 = 0.088 μM. | 16415863 | |
| BA/F3 | Growth inhibition assay | 48 hrs | Growth inhibition of mouse BA/F3 cells expressing wild-type Bcr-Abl after 48 hrs by MTT assay, IC50 = 0.089 μM. | 26562217 | ||
| K562 | Function assay | 30 mins | Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.09 μM. | 28280261 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0905 μM. | 30137981 | ||
| BA/F3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against mouse BA/F3 cells transfected with wild type Bcr-Abl after 48 hrs by XTT assay, IC50 = 0.092 μM. | 23600806 | ||
| GIST882 | Function assay | Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA, IC50 = 0.097 μM. | 20817538 | |||
| GIST882 | Function assay | Inhibition of KIT K642E mutant autophosphorylation (unknown origin) expressed in human GIST882 cells by ELISA, IC50 = 0.097 μM. | 23611771 | |||
| insect | Function assay | 30 mins | Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0982 μM. | 23301703 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 0.1 μM. | 19301902 | ||
| primary leukemia cells | Cytotoxicity assay | 72 hrs | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.1 μM. | 22221201 | ||
| BV173 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human BV173 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.1 μM. | 27011159 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.1 μM. | 27077705 | ||
| K562 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human K562 cells after 24 hrs by MTT assay, IC50 = 0.1 μM. | 22632935 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.102 μM. | 30204441 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused c-KIT L576P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.102 μM. | 27966954 | ||
| GIST882 | Antiproliferative assay | Antiproliferative activity against human GIST882 cells, IC50 = 0.108 μM. | 20817538 | |||
| GIST882 | Function assay | Inhibition of KIT K642E mutant (unknown origin) expressed in human GIST882 cells assessed as cell growth inhibition by ATP-depletion assay, IC50 = 0.108 μM. | 23611771 | |||
| K562 | Cytotoxicity assay | Cytotoxic effect in K562 cells, IC50 = 0.11 μM. | 12951113 | |||
| KU812 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KU812 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.11 μM. | 28541695 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay, IC50 = 0.11 μM. | 23088644 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused CSF1R (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.11 μM. | 27966954 | ||
| 32D | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse 32D cells transfected with p210 cells expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay, IC50 = 0.112 μM. | 16415863 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.1143 μM. | 23301703 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.115 μM. | 23301703 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.12 μM. | 27077705 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay, IC50 = 0.129 μM. | 23088644 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.14 μM. | 26789553 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA, IC50 = 0.141 μM. | 20817538 | |||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.147 μM. | 28541695 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT A829P mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.1482 μM. | 28541695 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.149 μM. | 30137981 | ||
| KU812 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.16 μM. | 26789553 | ||
| KU812 | Antiproliferative assay | 72 hrs | Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.16 μM. | 27077705 | ||
| A10 | Function assay | 68 hrs | Inhibition of PDGFR-beta driven proliferation of rat A10 cells after 68 hrs in presence of rat recombinant PDGF-BB by cell titer-glo luminescence assay, IC50 = 0.162 μM. | 27502700 | ||
| KU812 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.163 μM. | 27966954 | ||
| K562 | Cytotoxicity assay | Cytotoxicity against human K562 cells, IC50 = 0.17 μM. | 23600806 | |||
| K562 | Antiproliferative assay | Antiproliferative activity against human K562 cells, GI50 = 0.17 μM. | 22439674 | |||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.1739 μM. | 23301703 | ||
| K562 | Cytotoxicity assay | Cytotoxicity against K562 cells by MTT assay, IC50 = 0.18 μM. | 17572088 | |||
| K562 | Antiproliferative assay | Antiproliferative activity against K562 cells, IC50 = 0.182 μM. | 16332440 | |||
| 32D | Cytotoxicity assay | Cytotoxic activity against mouse 32D cells transfected with p210 Bcr-abl, IC50 = 0.19 μM. | 16415863 | |||
| BA/F3 | Antiproliferative assay | 48 hrs | Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.19 μM. | 16415863 | ||
| BA/F3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse BA/F3 cells transfected with p210 Bcr-abl assessed as proliferation after 48 hrs by MTT assay, IC50 = 0.19 μM. | 16415863 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.192 μM. | 30204441 | ||
| 32D | Function assay | Inhibition of human BCR-ABL1 (unknown origin) expressed in mouse 32D cells, IC50 = 0.194 μM. | 23611771 | |||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.2 μM. | 27011159 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.201 μM. | 30137981 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.216 μM. | 30204441 | ||
| Sf9 | Function assay | Inhibition of human Lyn kinase expressed in Sf9 cells, IC50 = 0.22 μM. | 17376680 | |||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by trypan blue dye exclusion assay, IC50 = 0.22 μM. | 26629859 | ||
| Ba/F | Function assay | Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells, IC50 = 0.221 μM. | 20817538 | |||
| BA/F3 | Function assay | Inhibition of human BCR-ABL1 autophosphorylation expressed in mouse BA/F3 cells by ELISA, IC50 = 0.221 μM. | 23611771 | |||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.223 μM. | 30204441 | ||
| SF9 | Function assay | 1 hr | Inhibition of C-terminal His-tagged human ABL1 expressed in baculovirus infected SF9 cells using Tyr 02 peptide as substrate measured after 1 hr by FRET based Z'Lyte assay, IC50 = 0.223 μM. | 27966954 | ||
| NCI-H1703 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1703 cells after 72 hrs in presence of PDGF-AA by CellTiter-Glo or CCK-8 assay, GI50 = 0.23 μM. | 29544149 | ||
| CHO | Function assay | Inhibition of wild type Platelet-derived growth factor receptor beta phosphorylation in CHO cells, IC50 = 0.24 μM. | 12166950 | |||
| MEG01 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.24 μM. | 26789553 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.24 μM. | 23301703 | ||
| K562 | Antiproliferative assay | Antiproliferative activity against human K562 cells, IC50 = 0.244 μM. | 20817538 | |||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.249 μM. | 30137981 | ||
| K562 | Function assay | 30 mins | Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.25 μM. | 28280261 | ||
| M07e | Antiproliferative assay | 48 hrs | Antiproliferative activity against human M07e Bcr-abl negative cells expressing stem cell factor assessed as proliferation after 48 hrs by MTT assay, IC50 = 0.257 μM. | 16415863 | ||
| CHO | Function assay | Inhibition of chimeric PDGF receptor with c-kit cytoplasmic domain phosphorylation in CHO cells, IC50 = 0.26 μM. | 12166950 | |||
| EM2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human EM2 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.26 μM. | 27011159 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.267 μM. | 27966954 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of human BCR/ABL p210 fusion protein expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.27 μM. | 27966954 | ||
| K562 | Function assay | 30 mins | Inhibition of kinobead binding to ARG in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.272 μM. | 28280261 | ||
| KBM5 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTT assay, IC50 = 0.28 μM. | 20149665 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.28 μM. | 26195136 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA, IC50 = 0.291 μM. | 20817538 | |||
| Sf9 | Function assay | Inhibition of recombinant Abl kinase (unknown origin) expressed in Sf9 cells using GGEAIYAAPFKK as substrate in presence of [gamma33P]ATP, IC50 = 0.3 μM. | 24681986 | |||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by XTT assay, IC50 = 0.31 μM. | 27214512 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.312 μM. | 30204441 | ||
| ALL3 | Cytotoxicity assay | Cytotoxicity against Philadelphia chromosome positive human ALL3 cells by Alamar Blue fluorescent assay, IC50 = 0.333 μM. | 19889540 | |||
| KU812 | Antiproliferative assay | Antiproliferative activity against human KU812 cells, IC50 = 0.337 μM. | 21376587 | |||
| BA/F3 | Antiproliferative assay | 48 hrs | Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A337N mutant assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.339 μM. | 16415863 | ||
| CML | Antiproliferative assay | Antiproliferative activity against human CML cells, IC50 = 0.35 μM. | 19219016 | |||
| HEK293 | Function assay | 1.5 mins | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay, IC50 = 0.35 μM. | 23241029 | ||
| HEK293 | Function assay | 1.5 mins | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50 = 0.35 μM. | 23241029 | ||
| M-NFS-60 | Antiproliferative assay | Antiproliferative activity against mouse M-NFS-60 cells, IC50 = 0.358 μM. | 20817538 | |||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.3599 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay, IC50 = 0.362 μM. | 23088644 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-fused c-KIT (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.37 μM. | 29544149 | ||
| BAF3 | Function assay | Inhibition of Tel-fused c-KIT (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.37 μM. | 27966954 | |||
| K562 | Antiproliferative assay | Antiproliferative activity against human K562 cells, IC50 = 0.38 μM. | 21376587 | |||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50 = 0.38 μM. | 26850004 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.38 μM. | 26789553 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.3819 μM. | 28541695 | ||
| K562 | Cytotoxicity assay | 48 to 72 hrs | Cytotoxicity against human BCR-ABL positive K562 cells after 48 to 72 hrs by MTT assay, IC50 = 0.3844 μM. | 22789429 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells after 72 hrs by MTS assay, GI50 = 0.39 μM. | 22932313 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.392 μM. | 30204441 | ||
| BA/F3 | Antiproliferative assay | 5 to 10 uM | 48 hrs | Antiproliferative activity against mouse BA/F3 cells expressing NPM-abl assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay, IC50 = 0.393 μM. | 16415863 | |
| K562 | Function assay | Inhibitory activity against human K562 cells growth using MTT assay, IC50 = 0.4 μM. | 14552760 | |||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.4 μM. | 27077705 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay, IC50 = 0.424 μM. | 23088644 | ||
| KCL22 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human KCL22 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay, GI50 = 0.43 μM. | 27011159 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.455 μM. | 30137981 | ||
| Sf9 | Function assay | Inhibition of human Abl kinase expressed in Sf9 cells, IC50 = 0.47 μM. | 17376680 | |||
| K562 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.47 μM. | 23735826 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.47 μM. | 25778766 | ||
| K562 | Function assay | Inhibition of BCR-ABL1 autophosphorylation in human K562 cells, IC50 = 0.473 μM. | 20817538 | |||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.4858 μM. | 23301703 | ||
| Sf9 | Function assay | Binding affinity to human remote site of N-terminal hexahistidine-tagged ABL2 expressed in Trichoplusia ni infected Sf9 cells by isothermal titration calorimetric assay, Kd = 0.5 μM. | 21417343 | |||
| primary leukemia cells | Cytotoxicity assay | 72 hrs | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.5 μM. | 22221201 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.5 μM. | 26789553 | ||
| K562 | Antiproliferative assay | Antiproliferative activity against human K562 cells, IC50 = 0.5 μM. | 23352483 | |||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells after 72 hrs by calcein-AM assay, IC50 = 0.5 μM. | 23981532 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells after 72 hrs using Calcein AM by fluorescence assay, IC50 = 0.5 μM. | 25757603 | ||
| K562 | Cytotoxicity assay | Cytotoxicity against human K562 cells, IC50 = 0.5 μM. | 27189674 | |||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.5 μM. | 23301703 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.5 μM. | 23932071 | ||
| Sf9 | Function assay | TP_TRANSPORTER: inhibition of ATPase activity in BCRP-expressing Sf9 cells, IC50 = 0.5 μM. | 15155841 | |||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.51 μM. | 26814890 | ||
| K562 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.53 μM. | 26707846 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.53 μM. | 28525838 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.535 μM. | 30204441 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.567 μM. | 30204441 | ||
| K562 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50 = 0.58 μM. | 21295380 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.59 μM. | 23301703 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.625 μM. | 26789553 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210 fusion protein M356T mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.625 μM. | 27966954 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.659 μM. | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.669 μM. | 30204441 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells, IC50 = 0.678 μM. | 20817538 | |||
| BA/F3 | Function assay | Inhibition of human BCR-ABL1 expressed in mouse BA/F3 cells assessed as cell growth inhibition by ATP-depletion assay, IC50 = 0.678 μM. | 23611771 | |||
| K562 | Apoptosis assay | 48 hrs | Induction of apoptosis in human K562 cells after 48 hrs by annexinV and propidium iodide staining based flow cytometry, AC50 = 0.68 μM. | 26629859 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.701 μM. | 30204441 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by fluorescence microplate reader method, IC50 = 0.73 μM. | 26741853 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of ABL in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 0.73 μM. | 28974338 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.7496 μM. | 23301703 | ||
| K562 | Function assay | 2 hrs | Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis, IC50 = 0.75 μM. | 20188579 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT V559D/V654A double mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.803 μM. | 28541695 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT V654A mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 0.8031 μM. | 28541695 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.836 μM. | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.838 μM. | 30137981 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210 fusion protein F317I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 0.85 μM. | 27966954 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.855 μM. | 26789553 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.874 μM. | 30137981 | ||
| Sf9 | Function assay | TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells, IC50 = 0.9 μM. | 15155841 | |||
| CHO | Function assay | Inhibition of chimeric PDGF receptor with CSF-1R cytoplasmic domain phosphorylation in CHO cells, IC50 = 0.96 μM. | 12166950 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay, IC50 = 0.96 μM. | 23088644 | ||
| BA/F3 | Antiproliferative assay | 48 hrs | Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A334l mutant assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.962 μM. | 16415863 | ||
| K562 | Cytotoxicity assay | 24 hrs | Cytotoxicity against imatinib-sensitive human K562 cells assessed as decrease in cell viability after 24 hrs by XTT assay, IC50 = 1 μM. | 30261468 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1 μM. | 23301703 | ||
| GIST430 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 1.1 μM. | 28991465 | ||
| K562 | Cytotoxicity assay | 48 hrs | Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay, IC50 = 1.1 μM. | 29655981 | ||
| IR-K562 | Cytotoxicity assay | Cytotoxicity against imatinib resistant human IR-K562 cells assessed as reduction in cell viability, IC50 = 1.1 μM. | 26264503 | |||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.16 μM. | 26231079 | ||
| K562 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.16 μM. | 26451772 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 1.191 μM. | 30204441 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT D816H mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 1.245 μM. | 28541695 | ||
| FDC-P1 | Function assay | 48 hrs | Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay, IC50 = 1.274 μM. | 20156689 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.29 μM. | 27077705 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused c-KIT N822K mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 1.29 μM. | 27966954 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay, IC50 = 1.444 μM. | 23088644 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TEL-fused cKIT N822K mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 1.466 μM. | 28541695 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 1.523 μM. | 30204441 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1.6 μM. | 23301703 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.69 μM. | 26789553 | ||
| GIST882 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human GIST882 cells after 96 hrs by SRB assay, IC50 = 1.7 μM. | 19469547 | ||
| GIST882 | Antiproliferative assay | 96 hrs | Antiproliferative activity against imatinib-susceptible human GIST882 cells harboring c-KIT K642E mutant after 96 hrs by SRB assay, IC50 = 1.7 μM. | 29724653 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210 fusion protein H369P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 1.79 μM. | 27966954 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 1.834 μM. | 23088644 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay, IC50 = 1.863 μM. | 23088644 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.93 μM. | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 2.1 μM. | 26789553 | ||
| NCI-H1703 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1703 cells after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 2.1 μM. | 29544149 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210 fusion protein F317L mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 2.16 μM. | 27966954 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 2.169 μM. | 26789553 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay, IC50 = 2.377 μM. | 23088644 | ||
| HGC27 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay, IC50 = 2.4 μM. | 19469547 | ||
| HGC27 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay, IC50 = 2.4 μM. | 29724653 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.49 μM. | 27077705 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused c-KIT V654A mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 2.49 μM. | 27966954 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay, IC50 = 2.547 μM. | 23088644 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 2.749 μM. | 30204441 | ||
| HEK293 | Function assay | 1.5 mins | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50 = 2.9 μM. | 23241029 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay, IC50 = 2.951 μM. | 23088644 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 3 μM. | 26789553 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 3 μM. | 27077705 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused c-KIT V559D/V654A double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 3 μM. | 27966954 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay, IC50 = 3.005 μM. | 23088644 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 3.3 μM. | 23301703 | ||
| MDCK | Function assay | Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50 = 3.38 μM. | 19932960 | |||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50 = 3.43 μM. | 29684708 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 3.6 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay, IC50 = 3.763 μM. | 23088644 | ||
| HGC27 | Cytotoxicity assay | 48 hrs | Cytotoxicity against HGC27 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 3.8 μM. | 24900584 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 3.947 μM. | 30204441 | ||
| MCF7 MX | Function assay | Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining, IC50 = 4.07 μM. | 19932960 | |||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 4.1 μM. | 26789553 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against Bcr/Abl positive human K562 cells after 48 hrs by MTT method, IC50 = 4.12 μM. | 25464886 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 4.12 μM. | 26298495 | ||
| HEK293 | Function assay | 3 mins | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 4.2 μM. | 23241029 | ||
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 4.56 μM. | 28525838 | ||
| K562/G | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562/G cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 4.65 μM. | 26814890 | ||
| BAF3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 4.686 μM. | 28541695 | ||
| BA/F3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against mouse BA/F3 cells transfected with Bcr-Abl T315I mutant after 48 hrs by XTT assay, IC50 = 4.79 μM. | 23600806 | ||
| MCF7 | Function assay | Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay, IC50 = 4.89779 μM. | 18678495 | |||
| Sf9 | Function assay | Binding affinity to recombinant full length human N-terminal GST-tagged Syk-KD (356 to 635 residues) cytoplasmic domain expressed in baculovirus infected Sf9 insect cells using poly EY 4:1 as substrate, Ki = 5 μM. | 29132752 | |||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 5.155 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 5.2 μM. | 23301703 | ||
| HEL | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 5.3 μM. | 26789553 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 5.4 μM. | 21576023 | ||
| KBM5 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTT assay, IC50 = 5.4 μM. | 20149665 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 5.6 μM. | 23301703 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 6.67 μM. | 27077705 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of Tel-fused c-KIT T670I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay, GI50 = 6.67 μM. | 27966954 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 6.7 μM. | 26789553 | ||
| GIST48B | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GIST48B cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, GI50 = 6.986 μM. | 28541695 | ||
| BaF3 | Antiproliferative assay | Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay, IC50 = 7.1 μM. | 16970400 | |||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 7.12 μM. | 29684708 | ||
| A2780 | Function assay | Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50 = 7.24436 μM. | 18678495 | |||
| A2780/ADR | Function assay | Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay, IC50 = 7.24436 μM. | 17890094 | |||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 7.7 μM. | 26789553 | ||
| HEK293 | Cytotoxicity assay | Cytotoxicity against HEK293 cells assessed as reduction in cell viability, CC50 = 8.4 μM. | 26264503 | |||
| FDC-P1 | Function assay | 48 hrs | Inhibition of mouse GM-CSF-stimulated cell proliferation of growth factor dependent mouse FDC-P1 cells expressing human FMS after 48 hrs by resazurin dye reduction assay, IC50 = 8.437 μM. | 20156689 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay, IC50 = 8.615 μM. | 23088644 | ||
| A2780 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50 = 8.9 μM. | 29684708 | ||
| BESM | Antitrypanosomal assay | 88 hrs | Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50 = 9 μM. | 20547819 | ||
| BaF3 | Antiproliferative assay | Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay, IC50 = 9.1 μM. | 16970400 | |||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 9.2 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3, IC50 = 9.459 μM. | 20817538 | |||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 9.5 μM. | 23301703 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 9.645 μM. | 30137981 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 9.7 μM. | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 9.93 μM. | 30204441 | ||
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 10 μM. | 19301902 | ||
| HepG2 | Antiproliferative assay | 24 to 96 hrs | Antiproliferative activity against human HepG2 cells after 24 to 96 hrs by MTS assay, IC50 = 10 μM. | 23932071 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 11.1 μM. | 23301703 | ||
| MCF7 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 11.3 μM. | 29724653 | ||
| MCF7 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 11.5 μM. | 19469547 | ||
| RKOp21 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 12 μM. | 19301902 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 12.2 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 12.2 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 12.5 μM. | 23301703 | ||
| RKOp21 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 12.5892 μM. | 19301902 | ||
| K562 | Antiproliferative assay | 24 hrs | In vitro antiproliferative activity against human K562 cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50 = 13 μM. | 24681986 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 13.5 μM. | 23301703 | ||
| U937 | Antiproliferative assay | Antiproliferative activity against U937 cells, IC50 = 14 μM. | 16332440 | |||
| BA/F3 | Growth inhibition assay | 48 hrs | Growth inhibition of mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 48 hrs by MTT assay, IC50 = 14.5 μM. | 26562217 | ||
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 15.5 μM. | 19301902 | ||
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against imatinib-resistant human K562 cells after 48 hrs by MTT assay, IC50 = 15.7 μM. | 26231079 | ||
| MDA-MB-468 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 15.8489 μM. | 19301902 | ||
| KG1a | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KG1a cells assessed as inhibition of cell survival after 72 hrs by MTT assay, IC50 = 16.7 μM. | 26850004 | ||
| MDA-MB-468 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 17 μM. | 19301902 | ||
| HMC-1.2 | Antiproliferative assay | Antiproliferative activity against human HMC-1.2 cells carrying V560G, D816V mutant assessed as cell growth inhibition by MTT assay, IC50 = 17 μM. | 25004409 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay, IC50 = 17.083 μM. | 23088644 | ||
| HUVEC | Antiproliferative assay | Antiproliferative activity against HUVEC cells, GI50 = 18.5 μM. | 22439674 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay, IC50 = 18.52 μM. | 23088644 | ||
| HeLa | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay, IC50 = 18.65 μM. | 19301902 | ||
| GIST48 | Cytotoxicity assay | 3 to 6 days | Cytotoxicity against human GIST48 cells assessed as effect on cell viability after 3 to 6 days by luciferase based luminescence assay, IC50 = 18.7 μM. | 19469547 | ||
| Hec1A | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay, IC50 = 19 μM. | 19301902 | ||
| U937 | Cytotoxicity assay | Cytotoxicity against human U937 cells assessed as reduction in cell viability, IC50 = 19 μM. | 26264503 | |||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 19.66 μM. | 29684708 | ||
| GIST48 | Antiproliferative assay | 96 hrs | Antiproliferative activity against imatinib-resistant human GIST48 cells harboring c-KIT V560D/D820A double mutant after 96 hrs by SRB assay, IC50 = 19.8 μM. | 29724653 | ||
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 19.9526 μM. | 19301902 | ||
| CAL27 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 19.9526 μM. | 19301902 | ||
| Hec1A | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay, IC50 = 19.9526 μM. | 19301902 | ||
| 32D | Cytotoxicity assay | Cytotoxic activity against mouse 32D Bcr-abl negative cells, IC50 = 20 μM. | 16415863 | |||
| GIST48B | Growth inhibition assay | 72 hrs | Growth inhibition of human GIST48B cells after 72 hrs by SRB assay, GI50 = 20 μM. | 23773153 | ||
| BV173 | Antiproliferative assay | 24 hrs | In vitro antiproliferative activity against human BV173 cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50 = 20 μM. | 24681986 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of ABL T315I mutant in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 20.03 μM. | 28974338 | ||
| 293T | Cytotoxicity assay | Cytotoxicity against human 293T cells assessed as growth inhibition, CC50 = 20.53 μM. | 26850004 | |||
| CAL27 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 22 μM. | 19301902 | ||
| H460 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 24 μM. | 19301902 | ||
| PC3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 24 μM. | 19301902 | ||
| HCT15 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25 μM. | 19301902 | ||
| THP1 | Cytotoxicity assay | Cytotoxicity against human THP1 cells assessed as reduction in cell viability, IC50 = 25 μM. | 26264503 | |||
| HeLa | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. | 19301902 | ||
| H460 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. | 19301902 | ||
| HCT15 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. | 19301902 | ||
| PC3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. | 19301902 | ||
| Saos2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 25.1189 μM. | 19301902 | ||
| HEK293 | Function assay | 3 mins | Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 25.5 μM. | 23241029 | ||
| Saos2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 26 μM. | 19301902 | ||
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 30 μM. | 19301902 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 31 μM. | 19301902 | ||
| H69 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 31.6228 μM. | 19301902 | ||
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 31.6228 μM. | 19301902 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 31.6228 μM. | 19301902 | ||
| H69 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 32 μM. | 19301902 | ||
| BESM | Cytotoxicity assay | 88 hrs | Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50 = 32 μM. | 20547819 | ||
| HCT116 | Anticancer assay | Anticancer activity against human HCT116 cells, IC50 = 34.4 μM. | 26312434 | |||
| CCRF-CEM | Cytotoxicity assay | 72 hrs | Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay, IC50 = 36 μM. | 19301902 | ||
| MDA-MB-231 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 37 μM. | 19301902 | ||
| CCRF-CEM/VCR1000 | Cytotoxicity assay | 72 hrs | Cytotoxicity against vincristine-resistant human CCRF-CEM/VCR1000 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 37 μM. | 19301902 | ||
| WM266.4 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 37 μM. | 19301902 | ||
| U87MG | Cytotoxicity assay | 72 hrs | Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay, IC50 = 38 μM. | 19301902 | ||
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39 μM. | 19301902 | ||
| MDA-MB-231 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. | 19301902 | ||
| SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. | 19301902 | ||
| AsPC1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. | 19301902 | ||
| CCRF-CEM/VCR1000 | Cytotoxicity assay | 72 hrs | Cytotoxicity against vincristine-resistant human CCRF-CEM/VCR1000 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. | 19301902 | ||
| CCRF-CEM | Cytotoxicity assay | 72 hrs | Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. | 19301902 | ||
| U87MG | Cytotoxicity assay | 72 hrs | Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. | 19301902 | ||
| WM266.4 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 39.8107 μM. | 19301902 | ||
| AsPC1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 44 μM. | 19301902 | ||
| CCRF-CEM | Antiproliferative assay | 24 hrs | In vitro antiproliferative activity against human CCRF-CEM cells assessed as decrease in cell viability after 24 hrs by MTT assay, IC50 = 45 μM. | 24681986 | ||
| A2780 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A2780 cells after 72 hrs by alamar-blue cell viability assay, IC50 = 48 μM. | 19301902 | ||
| Vero | Antiviral assay | 3 days | Antiviral activity against Dengue virus infected in african green monkey Vero cells administered before viral challenge after 3 days by viral plaque assay | 17360676 | ||
| Ba/F3 | Function assay | 1 uM | 24 hrs | Inhibition of 14-3-3sigma in human Ba/F3 cells expressing wild type Bcr-Abl construct assessed as release of full-length c-Abl from cytoplasmic complex with 14-3-3sigma at 1 uM after 24 hrs by immunoprecipitation/immunoblot technique | 21962576 | |
| Ba/F3 | Function assay | 1 uM | 24 hrs | Inhibition of 14-3-3sigma in human Ba/F3 cells expressing wild type Bcr-Abl construct assessed as nuclear import of full-length c-Abl at 1 uM after 24 hrs by immunoprecipitation/immunoblot technique | 21962576 | |
| Neuro2a | Function assay | 1 uM | Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 26789657 | ||
| K562 | Function assay | 100 uM | 8 hrs | Inhibition of BCR-ABL signaling pathway in human K562 cells assessed as suppression of STAT5 phosphorylation at 100 uM after 8 hrs in presence of MeBS by Western blot analysis | 27666635 | |
| K562 | Function assay | 100 uM | 8 hrs | Inhibition of BCR-ABL in signaling pathway human K562 cells assessed as suppression of CrkL phosphorylation at 100 uM after 8 hrs in presence of MeBS by Western blot analysis | 27666635 | |
| K562 | Function assay | 100 uM | 8 hrs | Inhibition of BCR-ABL phosphorylation in human K562 cells at 100 uM after 8 hrs in presence of MeBS by Western blot analysis | 27666635 | |
| K562 | Function assay | 10 uM | 1 hr | Inhibition of tyrosine phosphorylation of protein with molecular weight between 40 and 60 kDa in human K562 cells at 10 uM after 1 hr by immunoblot analysis | 24681986 | |
| K562 | Function assay | 10 uM | 1 hr | Inhibition of Bcr/Abl kinase tyrosine phosphorylation in human K562 cells at 10 uM after 1 hr by immunoblot analysis | 24681986 | |
| K562 | Function assay | 10 uM | 1 hr | Inhibition of Abl kinase tyrosine phosphorylation in human K562 cells at 10 uM after 1 hr by immunoblot analysis | 24681986 | |
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | |||
| NCI-H1703 | Function assay | 1 uM | 2 hrs | Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y754 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 29544149 | |
| NCI-H1703 | Function assay | 1 uM | 2 hrs | Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y1018 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 29544149 | |
| NCI-H1703 | Function assay | 1 uM | 2 hrs | Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y849 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 29544149 | |
| EOL-1 | Function assay | 1 uM | 2 hrs | Inhibition of PDGFRalpha in human EOL-1 cells assessed as decrease in STAT5 phosphorylation at Y694 residue at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 29544149 | |
| EOL-1 | Function assay | 1 uM | 2 hrs | Inhibition of PDGFRalpha in human EOL-1 cells assessed as decrease in ERK phosphorylation at T202/Y204 residues at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 29544149 | |
| K562 | Function assay | 1 uM | Inhibition of BCR-ABL in imatinib-sensitive human K562 cells assessed as decrease in CrKL phosphorylation at 1 uM by immuno blot analysis | 30261468 | ||
| BA/F3 | Antitumor assay | 50 mg/kg | 14 days | Antitumor activity against mouse BA/F3 cells expressing wild type BCR-ABL allografted in SCID mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 14 days | 23301703 | |
| Ba/F3 | Function assay | 1 hr | Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated STAT5 level after 1 hr by Western blot analysis | 23600806 | ||
| Ba/F3 | Function assay | 1 hr | Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated CrkL level after 1 hr by Western blot analysis | 23600806 | ||
| Ba/F3 | Function assay | 1 hr | Inhibition of Bcr-Abl T315I mutant (unknown origin) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis | 23600806 | ||
| K562 | Function assay | 6 hrs | Inhibition of BCR-ABL-mediated STAT5 phosphorylation in human K562 cells after 6 hrs by phospho-flow cytometry | 22148584 | ||
| K562 | Function assay | 40 uM | 6 hrs | Inhibition of BCR-ABL-mediated ERK1 phosphorylation in human K562 cells at 40 uM after 6 hrs by phospho-flow cytometry | 22148584 | |
| K562 | Function assay | 40 uM | 6 hrs | Inhibition of BCR-ABL-mediated ERK2 phosphorylation in human K562 cells at 40 uM after 6 hrs by phospho-flow cytometry | 22148584 | |
| GISTT1 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT autophosphorylation at Y719 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GISTT1 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT autophosphorylation at Y823 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GISTT1 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT autophosphorylation at Y703 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GIST882 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT autophosphorylation at Y823 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GIST882 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT autophosphorylation at Y703 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GIST882 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT autophosphorylation at Y719 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GISTT1 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphorylation at S473 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GISTT1 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phosphorylation at Y705/Y694 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GISTT1 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosphorylation at T202/Y204 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GISTT1 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6 phosphorylation at S235/236 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GIST882 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6 phosphorylation at S235/236 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GIST882 | Cell cycle assay | 1 uM | 48 hrs | Cell cycle arrest in human GIST882 cells assessed as accumulation at G0/G1 phase at 1 uM after 48 hrs by propidium iodide/RNase staining based flow cytometry | 27966954 | |
| K562 | Apoptosis assay | 1 uM | Induction of apoptosis in human K562 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 27966954 | ||
| K562 | Apoptosis assay | 1 uM | Induction of apoptosis in human K562 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 27966954 | ||
| K562 | Cell cycle assay | 1 uM | 24 hrs | Cell cycle arrest in human K562 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry | 27966954 | |
| GISTT1 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphorylation at T389 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| KU812 | Apoptosis assay | 1 uM | Induction of apoptosis in human KU812 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 27966954 | ||
| GIST882 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phosphorylation at Y705/Y694 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| KU812 | Apoptosis assay | 1 uM | Induction of apoptosis in human KU812 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 27966954 | ||
| GIST882 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosphorylation at T202/Y204 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| GIST882 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphorylation at T389 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| KU812 | Cell cycle assay | 1 uM | 12 hrs | Cell cycle arrest in human KU812 cells assessed as accumulation at G0/G1 phase at 1 uM after 12 hrs by propidium iodide/RNase staining based flow cytometry | 27966954 | |
| MEG01 | Apoptosis assay | 1 uM | Induction of apoptosis in human MEG01 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 27966954 | ||
| GISTT1 | Apoptosis assay | 1 uM | Induction of apoptosis in human GISTT1 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 27966954 | ||
| GIST882 | Apoptosis assay | 1 uM | Induction of apoptosis in human GIST882 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 27966954 | ||
| GIST882 | Apoptosis assay | 1 uM | Induction of apoptosis in human GIST882 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 27966954 | ||
| MEG01 | Cell cycle assay | 1 uM | 24 hrs | Cell cycle arrest in human MEG01 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry | 27966954 | |
| GISTT1 | Cell cycle assay | 1 uM | 24 hrs | Cell cycle arrest in human GISTT1 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry | 27966954 | |
| MEG01 | Apoptosis assay | 1 uM | Induction of apoptosis in human MEG01 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 27966954 | ||
| GISTT1 | Apoptosis assay | 1 uM | Induction of apoptosis in human GISTT1 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 27966954 | ||
| GIST882 | Function assay | 1 uM | 2 hrs | Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphorylation at S473 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 27966954 | |
| LAMA-84 | Growth Inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50 = 0.07304 μM. | SANGER | |||
| EM-2 | Growth Inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay, IC50 = 0.0888 μM. | SANGER | |||
| MEG-01 | Growth Inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay, IC50 = 0.08921 μM. | SANGER | |||
| BV-173 | Growth Inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay, IC50 = 0.1874 μM. | SANGER | |||
| K-562 | Growth Inhibition assay | Inhibition of human K-562 cell growth in a cell viability assay, IC50 = 0.22432 μM. | SANGER | |||
| CGTH-W-1 | Growth Inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 0.38374 μM. | SANGER | |||
| ST486 | Growth Inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50 = 0.6854 μM. | SANGER | |||
| NCI-H1436 | Growth Inhibition assay | Inhibition of human NCI-H1436 cell growth in a cell viability assay, IC50 = 0.97801 μM. | SANGER | |||
| NOS-1 | Growth Inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50 = 1.65383 μM. | SANGER | |||
| A498 | Growth Inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50 = 2.57223 μM. | SANGER | |||
| BE-13 | Growth Inhibition assay | Inhibition of human BE-13 cell growth in a cell viability assay, IC50 = 2.62106 μM. | SANGER | |||
| SUP-T1 | Growth Inhibition assay | Inhibition of human SUP-T1 cell growth in a cell viability assay, IC50 = 3.82907 μM. | SANGER | |||
| NCI-H1770 | Growth Inhibition assay | Inhibition of human NCI-H1770 cell growth in a cell viability assay, IC50 = 5.57262 μM. | SANGER | |||
| IMR-5 | Growth Inhibition assay | Inhibition of human IMR-5 cell growth in a cell viability assay, IC50 = 6.22147 μM. | SANGER | |||
| LB2241-RCC | Growth Inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50 = 8.07384 μM. | SANGER | |||
| TGBC24TKB | Growth Inhibition assay | Inhibition of human TGBC24TKB cell growth in a cell viability assay, IC50 = 8.34052 μM. | SANGER | |||
| SCC-15 | Growth Inhibition assay | Inhibition of human SCC-15 cell growth in a cell viability assay, IC50 = 10.7788 μM. | SANGER | |||
| BB49-HNC | Growth Inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50 = 14.3335 μM. | SANGER | |||
| ES7 | Growth Inhibition assay | Inhibition of human ES7 cell growth in a cell viability assay, IC50 = 14.7379 μM. | SANGER | |||
| LB2518-MEL | Growth Inhibition assay | Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50 = 16.6094 μM. | SANGER | |||
| NCI-H510A | Growth Inhibition assay | Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50 = 17.2442 μM. | SANGER | |||
| TE-441-T | Growth Inhibition assay | Inhibition of human TE-441-T cell growth in a cell viability assay, IC50 = 17.2886 μM. | SANGER | |||
| HH | Growth Inhibition assay | Inhibition of human HH cell growth in a cell viability assay, IC50 = 17.3999 μM. | SANGER | |||
| LC4-1 | Growth Inhibition assay | Inhibition of human LC4-1 cell growth in a cell viability assay, IC50 = 18.0652 μM. | SANGER | |||
| KARPAS-45 | Growth Inhibition assay | Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50 = 18.1848 μM. | SANGER | |||
| LB1047-RCC | Growth Inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50 = 18.4452 μM. | SANGER | |||
| NKM-1 | Growth Inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50 = 19.3552 μM. | SANGER | |||
| SCLC-21H | Growth Inhibition assay | Inhibition of human SCLC-21H cell growth in a cell viability assay, IC50 = 20.1246 μM. | SANGER | |||
| RS4-11 | Growth Inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 20.3308 μM. | SANGER | |||
| ALL-PO | Growth Inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50 = 20.8149 μM. | SANGER | |||
| GDM-1 | Growth Inhibition assay | Inhibition of human GDM-1 cell growth in a cell viability assay, IC50 = 22.5945 μM. | SANGER | |||
| DMS-79 | Growth Inhibition assay | Inhibition of human DMS-79 cell growth in a cell viability assay, IC50 = 24.4934 μM. | SANGER | |||
| MPP-89 | Growth Inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 25.6874 μM. | SANGER | |||
| NB10 | Growth Inhibition assay | Inhibition of human NB10 cell growth in a cell viability assay, IC50 = 26.47 μM. | SANGER | |||
| LS-513 | Growth Inhibition assay | Inhibition of human LS-513 cell growth in a cell viability assay, IC50 = 26.8847 μM. | SANGER | |||
| L-540 | Growth Inhibition assay | Inhibition of human L-540 cell growth in a cell viability assay, IC50 = 26.9143 μM. | SANGER | |||
| ES1 | Growth Inhibition assay | Inhibition of human ES1 cell growth in a cell viability assay, IC50 = 27.521 μM. | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50 = 30.5093 μM. | SANGER | |||
| EW-1 | Growth Inhibition assay | Inhibition of human EW-1 cell growth in a cell viability assay, IC50 = 32.9454 μM. | SANGER | |||
| Calu-6 | Growth Inhibition assay | Inhibition of human Calu-6 cell growth in a cell viability assay, IC50 = 33.1855 μM. | SANGER | |||
| CTV-1 | Growth Inhibition assay | Inhibition of human CTV-1 cell growth in a cell viability assay, IC50 = 33.9789 μM. | SANGER | |||
| YT | Growth Inhibition assay | Inhibition of human YT cell growth in a cell viability assay, IC50 = 38.5209 μM. | SANGER | |||
| TE-6 | Growth Inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay, IC50 = 41.2797 μM. | SANGER | |||
| HT-144 | Growth Inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay, IC50 = 41.5486 μM. | SANGER | |||
| EW-13 | Growth Inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50 = 42.2791 μM. | SANGER | |||
| KALS-1 | Growth Inhibition assay | Inhibition of human KALS-1 cell growth in a cell viability assay, IC50 = 43.1328 μM. | SANGER | |||
| MOLT-16 | Growth Inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50 = 45.0752 μM. | SANGER | |||
| D-336MG | Growth Inhibition assay | Inhibition of human D-336MG cell growth in a cell viability assay, IC50 = 45.9599 μM. | SANGER | |||
| TE-11 | Growth Inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay, IC50 = 46.653 μM. | SANGER | |||
| EB2 | Growth Inhibition assay | Inhibition of human EB2 cell growth in a cell viability assay, IC50 = 46.699 μM. | SANGER | |||
| SK-N-DZ | Growth Inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50 = 48.0961 μM. | SANGER | |||
| SW684 | Growth Inhibition assay | Inhibition of human SW684 cell growth in a cell viability assay, IC50 = 48.2695 μM. | SANGER | |||
| EW-18 | Growth Inhibition assay | Inhibition of human EW-18 cell growth in a cell viability assay, IC50 = 48.4395 μM. | SANGER | |||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
Informazioni chimiche, conservazione e stabilità
| Peso molecolare | 589.71 | Formula | C29H31N7O.CH4SO3 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 220127-57-1 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | CGP-57148B,STI571 | Smiles | CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5.CS(=O)(=O)O | ||
Solubilità
|
In vitro |
DMSO
: 118 mg/mL
(200.09 mM)
Water : 118 mg/mL Ethanol : Insoluble |
Calcolatore di Molarità
Calcolatore di Diluizione
Calcolatore del Peso Molecolare
|
In vivo |
|||||
Calcolatore di formulazione in vivo (Soluzione chiara)
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)
mg/kg
g
μL
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.
Meccanismo dazione
| Targets/IC50/Ki |
PDGFR
(Cell-free assay) 100 nM
c-Kit
(M-07e cells) 100 nM
v-Abl
(Cell-free assay) 600 nM
|
|---|---|
| In vitro |
I saggi in vitro per l'inibizione di un pannello di tirosina e serina/treonina protein chinasi mostrano che Imatinib Mesylate inibisce potentemente la tirosina chinasi v-Abl e PDGFR con una IC50 di 0,6 e 0,1 μM, rispettivamente. Questo composto inibisce l'attivazione SLF-dipendente dell'attività chinasica c-kit di tipo selvaggio con una IC50 per questi effetti di circa 0,1 μM, che è simile alla concentrazione richiesta per l'inibizione di PDGFR. Esibisce attività inibitoria della crescita sulla linea cellulare di carcinoide bronchiale umano NCI-H727 e sulla linea cellulare di carcinoide pancreatico umano BON-1 con una IC50 di 32,4 e 32,8 μM, rispettivamente. Uno studio recente mostra che questa sostanza chimica ha il potenziale di esercitare i suoi effetti antileucemici nella leucemia mieloide cronica down-regolando i canali K(+) hERG1, che sono altamente espressi nelle cellule leucemiche e sembrano di eccezionale importanza nel favorire la leucemogenesi. |
| Saggio chinasico |
attività chinasica del recettore PDGF
|
|
Il recettore PDGF viene immunoprecipitato da estratti cellulari BALB/c 3T3 con antisiero di coniglio anti-recettore PDGF murino per 2 ore su ghiaccio. Vengono utilizzate perline di Proteina A-Sepharose per raccogliere i complessi antigene-anticorpo. Gli immunoprecipitati vengono lavati due volte con TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), una volta con TNE (50 mM Tris, pH 7.5, 140 mM EDTA), e una volta con tampone chinasi (20 mM Tris, pH 7.5, 10 mM MgCl2). Dopo stimolazione con PDGF (50 ng/mL) per 10 minuti a 4 °C, diverse concentrazioni di questo composto vengono aggiunte alla miscela di reazione. L'attività chinasica del recettore PDGF viene determinata mediante incubazione con 10 μCi [7-33P]-ATP e 1 μM ATP per 10 minuti a 4 °C. I complessi immuni vengono separati mediante SDS-PAGE su gel al 7,5%.
|
|
| In vivo |
Imatinib Mesylate produce un diverso effetto antitumorale su tre tumori xenotrapiantati derivati da campioni chirurgici di tumori polmonari a piccole cellule umani freschi, con l'80%, il 40% e il 78% di inibizione della crescita dei tumori SCLC6, SCLC61 e SCLC108, rispettivamente, e nessuna inibizione significativa della crescita di SCLC74. In topi ApoE(-/-) alimentati con dieta ricca di grassi, questo composto riduce significativamente l'area di colorazione lipidica indotta da grassi del 30%, 27% e 35% rispetto ai controlli non trattati con dieta ricca di grassi quando somministrato per gavage a 10, 20 e 40 mg/kg, rispettivamente, e sopprime l'accumulo di lipidi nell'arteria carotide. |
Riferimenti |
|
Applicazioni
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | p-ZAP70 / ZAP70 / p-LAT / LAT p-STAT3 / STAT3 / p-STAT5 / STAT5 |
|
18981115 |
| Immunofluorescence | Cortactin / F-actin RelB |
|
20937825 |
| Growth inhibition assay | Cell viability |
|
28435223 |
Informazioni sullo studio clinico
(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT05623774 | Recruiting | CML |
Inhibikase Therapeutics Inc. |
December 16 2022 | Phase 1 |
| NCT02687425 | Unknown status | Leukemia Myelogenous Chronic BCR-ABL Positive |
Meng Li|Tongji Hospital |
February 2016 | Phase 2 |
| NCT02303899 | Completed | Mesothelioma Malignant |
Istituto Clinico Humanitas |
November 2014 | Phase 2 |
| NCT01898377 | Terminated | Chronic Graft-versus-host Disease |
Seoul National University Hospital |
August 2013 | Phase 2 |
| NCT02891395 | Completed | Graft Versus Host Disease |
University Hospital Lille|Novartis |
December 24 2012 | Phase 2 |
Supporto tecnico
Istruzioni per la manipolazione
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