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Dasatinib Monohydrate Src inibitore
N. Cat.S7782
Struttura chimica
Peso molecolare: 506.02
Vai a
Controllo Qualità
Lotto:
Purezza:
99.62%
99.62
| Target correlati | EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl |
|---|---|
| Altro Src Inibitori | WH-4-023 Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 1-Naphthyl PP1(1-NA-PP1) RK 24466 |
Coltura cellulare, trattamento e concentrazione di lavoro
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | PMID |
|---|---|---|---|---|---|---|
| K562 cell | Proliferation assay | 72 h | Antiproliferative activity against human K562 cells after 72 hrs, IC50=0.001 μM | |||
| WiDr cell | Proliferation assay | 72 h | Antiproliferative activity against human WiDr cells after 72 hrs, IC50=0.052 μM | |||
| PC3 cell | Proliferation assay | 72 h | Antiproliferative activity against human PC3 cells after 72 hrs, IC50=0.0094 μM | |||
| MDA-MB-231 cell | Proliferation assay | 72 h | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs, IC50=0.012 μM | |||
| M07ep210 cell | Growth inhibition assay | 48 h | Growth inhibition of human M07ep210 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.07 nM | |||
| K562 cell | Growth inhibition assay | 48 h | Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.001 μM | |||
| M07e cell | Growth inhibition assay | 48 h | Growth inhibition of human M07e cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.0012 μM | |||
| K562 cell | Cytotoxicity assay | 72 h | Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=12.83 μM | |||
| U937 cell | Cytotoxicity assay | 72 h | Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=13.63 μM | |||
| K562 cell | Proliferation assay | 72 h | Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50=0.7 nM | |||
| MDA-MB-435S cell | Proliferation assay | 72 h | Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50=3.9 μM | |||
| NCI-H460 cell | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50=8.99 μM | |||
| NCI-H23 cell | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50=2.27 μM | |||
| A549 cell | Proliferation assay | 72 h | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=12.66 μM | |||
| T47D cell | Proliferation assay | 72 h | Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50=0.9 μM | |||
| HCT116 cell | Proliferation assay | 72 h | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=2.3 μM | |||
| MCF7 cells | Proliferation assay | 72 h | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=2.57 μM | |||
| RXF 393NL cell | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining, IC50=21.7 nM | |||
| PRXF DU145 cell | Cytotoxicity assay | 4 days | Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining, IC50=0.0623 μM | |||
| LXFA 983L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 983L cells after 4 days by propidium iodide staining, IC50=56.5 nM | |||
| GXF251L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining, IC50=2.25 μM | |||
| CXF 1103L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human CXF 1103L cells after 4 days by propidium iodide staining, IC50=4.36 μM | |||
| PAXF 1657L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining, IC50=0.121 μM | |||
| NCI-H1648 cell | Growth inhibition assay | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.02011 μM | ||||
| NCI-H1838 cell | Growth inhibition assay | Inhibition of human NCI-H1838 cell growth in a cell viability assay, IC50=1.30733 μM | ||||
| NCI-H2126 cell | Growth inhibition assay | Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=2.87552 μM | ||||
| NCI-H2141 cell | Growth inhibition assay | Inhibition of human NCI-H2141 cell growth in a cell viability assay, IC50=24.7754 μM | ||||
| NCI-H2107 cell | Growth inhibition assay | Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=43.4847 μM | ||||
| NCI-H747 cell | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=0.08362 μM | ||||
| NCI-H720 cell | Growth inhibition assay | Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=20.2733 μM | ||||
| NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay.IC50=1.30859 μM | ||||
| NMC-G1 cell | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay.IC50=0.11606 μM | ||||
| NTERA-S-cl-D1 cell | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay.IC50=0.12283 μM | ||||
| OCI-AML2 cell | Growth inhibition assay | Inhibition of human OCI-AML2 cell growth in a cell viability assay.IC50=5.86154 μM | ||||
| OCUB-M cell | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay.IC50=1.04412 μM | ||||
| OPM-2 cell | Growth inhibition assay | Inhibition of human OPM-2 cell growth in a cell viability assay.IC50=4.27685 μM | ||||
| OS-RC-2 cell | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay.IC50=0.0203 μM | ||||
| ONS-76 cell | Growth inhibition assay | Inhibition of human ONS-76 cell growth in a cell viability assay.IC50=0.42951 μM | ||||
| OVCAR-4 cell | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay.IC50=0.37433 μM | ||||
| NCI-H446 cell | Growth inhibition assay | Inhibition of human NCI-H446 cell growth in a cell viability assay.IC50=0.6276 μM | ||||
| NCI-H510A cell | Growth inhibition assay | Inhibition of human NCI-H510A cell growth in a cell viability assay.IC50=19.3973 μM | ||||
| PF-382 cell | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay.IC50=0.17678 μM | ||||
| NCI-H64 cell | Growth inhibition assay | Inhibition of human NCI-H64 cell growth in a cell viability assay.IC50=29.6253 μM | ||||
| PSN1 cell | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay.IC50=0.04474 μM | ||||
| QIMR-WIL cell | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay.IC50=0.70629 μM | ||||
| RL95-2 cell | Growth inhibition assay | Inhibition of human RL95-2 cell growth in a cell viability assay.IC50=0.1038 μM | ||||
| RCC10RGB cell | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay.IC50=0.4911 μM | ||||
| RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay.IC50=0.52966 μM | ||||
| NCI-SNU-16 cell | Growth inhibition assay | Inhibition of human NCI-SNU-16 cell growth in a cell viability assay.IC50=8.56128 μM | ||||
| RPMI-6666 cell | Growth inhibition assay | Inhibition of human RPMI-6666 cell growth in a cell viability assay.IC50=7.27067 μM | ||||
| NEC8 cell | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay.IC50=44.336 μM | ||||
| RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay.IC50=7.65787 μM | ||||
| RXF393 cell | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay.IC50=0.02357 μM | ||||
| Raji cell | Growth inhibition assay | Inhibition of human Raji cell growth in a cell viability assay.IC50=13.7497 μM | ||||
| NOS-1 cell | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay.IC50=0.006129 μM | ||||
| SBC-1 cell | Growth inhibition assay | Inhibition of human SBC-1 cell growth in a cell viability assay.IC50=1.57984 μM | ||||
| SF126 cell | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay.IC50=0.3541 μM | ||||
| SF539 cell | Growth inhibition assay | Inhibition of human SF539 cell growth in a cell viability assay.IC50=13.8557 μM | ||||
| SH-4 cell | Growth inhibition assay | Inhibition of human SH-4 cell growth in a cell viability assay.IC50=0.18413 μM | ||||
| OMC-1 cell | Growth inhibition assay | Inhibition of human OMC-1 cell growth in a cell viability assay.IC50=27.1422 μM | ||||
| SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay.IC50=9.02493 μM | ||||
| SJSA-1 cell | Growth inhibition assay | Inhibition of human SJSA-1 cell growth in a cell viability assay.IC50=8.72805 μM | ||||
| SK-LMS-1 cell | Growth inhibition assay | Inhibition of human SK-LMS-1 cell growth in a cell viability assay.IC50=3.11886 μM | ||||
| SK-NEP-1 cell | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay.IC50=8.89155 μM | ||||
| SKM-1 cell | Growth inhibition assay | Inhibition of human SKM-1 cell growth in a cell viability assay.IC50=9.01734 μM | ||||
| SK-PN-DW cell | Growth inhibition assay | Inhibition of human SK-PN-DW cell growth in a cell viability assay.IC50=36.1943 μM | ||||
| SK-UT-1 cell | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay.IC50=2.16693 μM | ||||
| SNB75 cell | Growth inhibition assay | Inhibition of human SNB75 cell growth in a cell viability assay.IC50=0.04435 μM | ||||
| REH cell | Growth inhibition assay | Inhibition of human REH cell growth in a cell viability assay.IC50=20.6357 μM | ||||
| SNU-C2B cell | Growth inhibition assay | Inhibition of human SNU-C2B cell growth in a cell viability assay.IC50=1.30589 μM | ||||
| RPMI-8866 cell | Growth inhibition assay | Inhibition of human RPMI-8866 cell growth in a cell viability assay.IC50=17.4455 μM | ||||
| SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay.IC50=0.04161 μM | ||||
| SW962 cell | Growth inhibition assay | Inhibition of human SW962 cell growth in a cell viability assay.IC50=0.11292 μM | ||||
| SF268 cell | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay.IC50=0.17404 μM | ||||
| TE-1 cell | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay.IC50=0.1054 μM | ||||
| 8-MG-BA cell | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay.IC50=0.15458 μM | ||||
| A101D cell | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay.IC50=1.03043 μM | ||||
| A253 cell | Growth inhibition assay | Inhibition of human A253 cell growth in a cell viability assay.IC50=3.73246 μM | ||||
| A3-KAW cell | Growth inhibition assay | Inhibition of human A3-KAW cell growth in a cell viability assay.IC50=0.98452 μM | ||||
| A4-Fuk cell | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay.IC50=38.1009 μM | ||||
| A388 cell | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay.IC50=0.05095 μM | ||||
| ACN cell | Growth inhibition assay | Inhibition of human ACN cell growth in a cell viability assay.IC50=1.82252 μM | ||||
| A704 cell | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay.IC50=0.01491 μM | ||||
| ALL-PO cell | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay.IC50=10.7938 μM | ||||
| ARH-77 cell | Growth inhibition assay | Inhibition of human ARH-77 cell growth in a cell viability assay.IC50=3.46915 μM | ||||
| SR cell | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay.IC50=4.49954 μM | ||||
| BB65-RCC cell | Growth inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay.IC50=0.08227 μM | ||||
| BB49-HNC cell | Growth inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay.IC50=0.38599 μM | ||||
| BC-1 cell | Growth inhibition assay | Inhibition of human BC-1 cell growth in a cell viability assay.IC50=28.651 μM | ||||
| BC-3 cell | Growth inhibition assay | Inhibition of human BC-3 cell growth in a cell viability assay.IC50=12.1138 μM | ||||
| BL-41 cell | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay.IC50=0.29123 μM | ||||
| BL-70 cell | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay.IC50=0.0000008218 μM | ||||
| SW684 cell | Growth inhibition assay | Inhibition of human SW684 cell growth in a cell viability assay.IC50=0.3498 μM | ||||
| BOKU cell | Growth inhibition assay | Inhibition of human BOKU cell growth in a cell viability assay.IC50=0.49133 μM | ||||
| SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay.IC50=0.02927 μM | ||||
| C2BBe1 cell | Growth inhibition assay | Inhibition of human C2BBe1 cell growth in a cell viability assay.IC50=0.08308 μM | ||||
| BV-173 cell | Growth inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay.IC50=0.000000109 μM | ||||
| Becker cell | Growth inhibition assay | Inhibition of human Becker cell growth in a cell viability assay.IC50=0.03003 μM | ||||
| SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay.IC50=0.01115 μM | ||||
| 697 cell | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay.IC50=0.19987 μM | ||||
| TE-15 cell | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay.IC50=0.005891 μM | ||||
| TE-11 cell | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay.IC50=0.07858 μM | ||||
| TE-5 cell | Growth inhibition assay | Inhibition of human TE-5 cell growth in a cell viability assay.IC50=1.79139 μM | ||||
| TE-6 cell | Growth inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay.IC50=1.21226 μM | ||||
| TE-9 cell | Growth inhibition assay | Inhibition of human TE-9 cell growth in a cell viability assay.IC50=0.87532 μM | ||||
| TGBC24TKB cell | Growth inhibition assay | Inhibition of human TGBC24TKB cell growth in a cell viability assay.IC50=0.04761 μM | ||||
| TGW cell | Growth inhibition assay | Inhibition of human TGW cell growth in a cell viability assay.IC50=11.2828 μM | ||||
| TK10 cell | Growth inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay.IC50=0.01174 μM | ||||
| TGBC1TKB cell | Growth inhibition assay | Inhibition of human TGBC1TKB cell growth in a cell viability assay.IC50=0.06164 μM | ||||
| A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay.IC50=0.07284 μM | ||||
| UACC-257 cell | Growth inhibition assay | Inhibition of human UACC-257 cell growth in a cell viability assay.IC50=12.9198 μM | ||||
| U-87-MG cell | Growth inhibition assay | Inhibition of human U-87-MG cell growth in a cell viability assay.IC50=30.766 μM | ||||
| BB30-HNC cell | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay.IC50=0.05437 μM | ||||
| no-10 cell | Growth inhibition assay | Inhibition of human no-10 cell growth in a cell viability assay.IC50=0.31931 μM | ||||
| CAS-1 cell | Growth inhibition assay | Inhibition of human CAS-1 cell growth in a cell viability assay.IC50=1.40992 μM | ||||
| CGTH-W-1 cell | Growth inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay.IC50=0.03548 μM | ||||
| TE-10 cell | Growth inhibition assay | Inhibition of human TE-10 cell growth in a cell viability assay.IC50=0.06357 μM | ||||
| COLO-684 cell | Growth inhibition assay | Inhibition of human COLO-684 cell growth in a cell viability assay.IC50=46.2258 μM | ||||
| TE-12 cell | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay.IC50=0.01861 μM | ||||
| COR-L279 cell | Growth inhibition assay | Inhibition of human COR-L279 cell growth in a cell viability assay.IC50=40.2852 μM | ||||
| TE-8 cell | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay.IC50=0.01576 μM | ||||
| CP66-MEL cell | Growth inhibition assay | Inhibition of human CP66-MEL cell growth in a cell viability assay.IC50=0.19531 μM | ||||
| CTV-1 cell | Growth inhibition assay | Inhibition of human CTV-1 cell growth in a cell viability assay.IC50=0.00004036 μM | ||||
| VA-ES-BJ cell | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay.IC50=0.03902 μM | ||||
| D-263MG cell | Growth inhibition assay | Inhibition of human D-263MG cell growth in a cell viability assay.IC50=0.36224 μM | ||||
| D-336MG cell | Growth inhibition assay | Inhibition of human D-336MG cell growth in a cell viability assay.IC50=0.006298 μM | ||||
| D-502MG cell | Growth inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay.IC50=1.23376 μM | ||||
| DJM-1 cell | Growth inhibition assay | Inhibition of human DJM-1 cell growth in a cell viability assay.IC50=6.48558 μM | ||||
| no-11 cell | Growth inhibition assay | Inhibition of human no-11 cell growth in a cell viability assay.IC50=0.50228 μM | ||||
| DMS-153 cell | Growth inhibition assay | Inhibition of human DMS-153 cell growth in a cell viability assay.IC50=14.0028 μM | ||||
| DSH1 cell | Growth inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay.IC50=0.24001 μM | ||||
| DU-4475 cell | Growth inhibition assay | Inhibition of human DU-4475 cell growth in a cell viability assay.IC50=8.21652 μM | ||||
| EB-3 cell | Growth inhibition assay | Inhibition of human EB-3 cell growth in a cell viability assay.IC50=34.3118 μM | ||||
| EHEB cell | Growth inhibition assay | Inhibition of human EHEB cell growth in a cell viability assay.IC50=10.0656 μM | ||||
| COLO-829 cell | Growth inhibition assay | Inhibition of human COLO-829 cell growth in a cell viability assay.IC50=0.12213 μM | ||||
| CP67-MEL cell | Growth inhibition assay | Inhibition of human CP67-MEL cell growth in a cell viability assay.IC50=0.20488 μM | ||||
| ES8 cell | Growth inhibition assay | Inhibition of human ES8 cell growth in a cell viability assay.IC50=32.1252 μM | ||||
| EVSA-T cell | Growth inhibition assay | Inhibition of human EVSA-T cell growth in a cell viability assay.IC50=9.27793 μM | ||||
| ES4 cell | Growth inhibition assay | Inhibition of human ES4 cell growth in a cell viability assay.IC50=1.05145 μM | ||||
| ETK-1 cell | Growth inhibition assay | Inhibition of human ETK-1 cell growth in a cell viability assay.IC50=0.02832 μM | ||||
| ES6 cell | Growth inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay.IC50=0.03193 μM | ||||
| EW-24 cell | Growth inhibition assay | Inhibition of human EW-24 cell growth in a cell viability assay.IC50=0.78165 μM | ||||
| EoL-1-cell cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay.IC50=0.00001309 μM | ||||
| Calu-6 cell | Growth inhibition assay | Inhibition of human Calu-6 cell growth in a cell viability assay.IC50=3.05741 μM | ||||
| GAK cell | Growth inhibition assay | Inhibition of human GAK cell growth in a cell viability assay.IC50=31.2686 μM | ||||
| D-247MG cell | Growth inhibition assay | Inhibition of human D-247MG cell growth in a cell viability assay.IC50=6.12519 μM | ||||
| GB-1 cell | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay.IC50=0.02157 μM | ||||
| GI-ME-N cell | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay.IC50=0.06118 μM | ||||
| GCIY cell | Growth inhibition assay | Inhibition of human GCIY cell growth in a cell viability assay.IC50=0.09656 μM | ||||
| GT3TKB cell | Growth inhibition assay | Inhibition of human GT3TKB cell growth in a cell viability assay.IC50=9.35546 μM | ||||
| HC-1 cell | Growth inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay.IC50=24.5551 μM | ||||
| HAL-01 cell | Growth inhibition assay | Inhibition of human HAL-01 cell growth in a cell viability assay.IC50=19.7543 μM | ||||
| HCC1187 cell | Growth inhibition assay | Inhibition of human HCC1187 cell growth in a cell viability assay.IC50=35.8052 μM | ||||
| DEL cell | Growth inhibition assay | Inhibition of human DEL cell growth in a cell viability assay.IC50=41.9086 μM | ||||
| HCC1599 cell | Growth inhibition assay | Inhibition of human HCC1599 cell growth in a cell viability assay.IC50=32.3325 μM | ||||
| DOHH-2 cell | Growth inhibition assay | Inhibition of human DOHH-2 cell growth in a cell viability assay.IC50=0.01719 μM | ||||
| HCC2157 cell | Growth inhibition assay | Inhibition of human HCC2157 cell growth in a cell viability assay.IC50=37.9946 μM | ||||
| HCE-4 cell | Growth inhibition assay | Inhibition of human HCE-4 cell growth in a cell viability assay.IC50=0.26439 μM | ||||
| HCE-T cell | Growth inhibition assay | Inhibition of human HCE-T cell growth in a cell viability assay.IC50=1.56714 μM | ||||
| HEL cell | Growth inhibition assay | Inhibition of human HEL cell growth in a cell viability assay.IC50=10.4776 μM | ||||
| EM-2 cell | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay.IC50=0.000001078 μM | ||||
| HT-144 cell | Growth inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay.IC50=0.53609 μM | ||||
| EW-16 cell | Growth inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay.IC50=0.76178 μM | ||||
| IA-LM cell | Growth inhibition assay | Inhibition of human IA-LM cell growth in a cell viability assay.IC50=12.4445 μM | ||||
| IST-MEL1 cell | Growth inhibition assay | Inhibition of human IST-MEL1 cell growth in a cell viability assay.IC50=0.1345 μM | ||||
| IST-MES1 cell | Growth inhibition assay | Inhibition of human IST-MES1 cell growth in a cell viability assay.IC50=0.08552 μM | ||||
| GI-1 cell | Growth inhibition assay | Inhibition of human GI-1 cell growth in a cell viability assay.IC50=1.3622 μM | ||||
| IST-SL2 cell | Growth inhibition assay | Inhibition of human IST-SL2 cell growth in a cell viability assay.IC50=0.50302 μM | ||||
| JVM-2 cell | Growth inhibition assay | Inhibition of human JVM-2 cell growth in a cell viability assay.IC50=2.36284 μM | ||||
| JVM-3 cell | Growth inhibition assay | Inhibition of human JVM-3 cell growth in a cell viability assay.IC50=37.2338 μM | ||||
| KALS-1 cell | Growth inhibition assay | Inhibition of human KALS-1 cell growth in a cell viability assay.IC50=0.0949 μM | ||||
| KARPAS-422 cell | Growth inhibition assay | Inhibition of human KARPAS-422 cell growth in a cell viability assay.IC50=0.33997 μM | ||||
| JiyoyeP-2003 cell | Growth inhibition assay | Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay.IC50=1.73466 μM | ||||
| KARPAS-45 cell | Growth inhibition assay | Inhibition of human KARPAS-45 cell growth in a cell viability assay.IC50=7.51671 μM | ||||
| KGN cell | Growth inhibition assay | Inhibition of human KGN cell growth in a cell viability assay.IC50=0.01942 μM | ||||
| KLE cell | Growth inhibition assay | Inhibition of human KLE cell growth in a cell viability assay.IC50=0.11317 μM | ||||
| KNS-42 cell | Growth inhibition assay | Inhibition of human KNS-42 cell growth in a cell viability assay.IC50=1.24412 μM | ||||
| KNS-81-FD cell | Growth inhibition assay | Inhibition of human KNS-81-FD cell growth in a cell viability assay.IC50=23.146 μM | ||||
| KP-N-YS cell | Growth inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay.IC50=12.9283 μM | ||||
| HOP-62 cell | Growth inhibition assay | Inhibition of human HOP-62 cell growth in a cell viability assay.IC50=0.01834 μM | ||||
| KURAMOCHI cell | Growth inhibition assay | Inhibition of human KURAMOCHI cell growth in a cell viability assay.IC50=0.03487 μM | ||||
| HUTU-80 cell | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay.IC50=0.3142 μM | ||||
| LAMA-84 cell | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay.IC50=0.000003207 μM | ||||
| LB1047-RCC cell | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay.IC50=0.009887 μM | ||||
| LB2518-MEL cell | Growth inhibition assay | Inhibition of human LB2518-MEL cell growth in a cell viability assay.IC50=0.14162 μM | ||||
| LB373-MEL-D cell | Growth inhibition assay | Inhibition of human LB373-MEL-D cell growth in a cell viability assay.IC50=0.82508 μM | ||||
| LB771-HNC cell | Growth inhibition assay | Inhibition of human LB771-HNC cell growth in a cell viability assay.IC50=2.57551 μM | ||||
| LB996-RCC cell | Growth inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay.IC50=0.009912 μM | ||||
| LC-2-ad cell | Growth inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay.IC50=0.02586 μM | ||||
| J-RT3-T3-5 cell | Growth inhibition assay | Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay.IC50=8.96529 μM | ||||
| LP-1 cell | Growth inhibition assay | Inhibition of human LP-1 cell growth in a cell viability assay.IC50=7.54782 μM | ||||
| K-562 cell | Growth inhibition assay | Inhibition of human K-562 cell growth in a cell viability assay.IC50=0.0000002656 μM | ||||
| LS-123 cell | Growth inhibition assay | Inhibition of human LS-123 cell growth in a cell viability assay.IC50=0.14064 μM | ||||
| K5 cell | Growth inhibition assay | Inhibition of human K5 cell growth in a cell viability assay.IC50=0.16489 μM | ||||
| LS-411N cell | Growth inhibition assay | Inhibition of human LS-411N cell growth in a cell viability assay.IC50=48.4748 μM | ||||
| KG-1 cell | Growth inhibition assay | Inhibition of human KG-1 cell growth in a cell viability assay.IC50=4.60845 μM | ||||
| KINGS-1 cell | Growth inhibition assay | Inhibition of human KINGS-1 cell growth in a cell viability assay.IC50=0.16666 μM | ||||
| LXF-289 cell | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay.IC50=0.03956 μM | ||||
| MC116 cell | Growth inhibition assay | Inhibition of human MC116 cell growth in a cell viability assay.IC50=0.1141 μM | ||||
| KS-1 cell | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay.IC50=0.0273 μM | ||||
| KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay.IC50=0.11883 μM | ||||
| MEG-01 cell | Growth inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay.IC50=0.000009805 μM | ||||
| MFH-ino cell | Growth inhibition assay | Inhibition of human MFH-ino cell growth in a cell viability assay.IC50=0.04724 μM | ||||
| L-540 cell | Growth inhibition assay | Inhibition of human L-540 cell growth in a cell viability assay.IC50=15.0671 μM | ||||
| MHH-NB-11 cell | Growth inhibition assay | Inhibition of human MHH-NB-11 cell growth in a cell viability assay.IC50=43.0818 μM | ||||
| MMAC-SF cell | Growth inhibition assay | Inhibition of human MMAC-SF cell growth in a cell viability assay.IC50=8.79307 μM | ||||
| LB2241-RCC cell | Growth inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay.IC50=9.02012 μM | ||||
| LB831-BLC cell | Growth inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay.IC50=0.04609 μM | ||||
| MOLT-16 cell | Growth inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay.IC50=29.6292 μM | ||||
| LC-1F cell | Growth inhibition assay | Inhibition of human LC-1F cell growth in a cell viability assay.IC50=27.3245 μM | ||||
| MOLT-4 cell | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay.IC50=26.6753 μM | ||||
| MZ1-PC cell | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay.IC50=0.03119 μM | ||||
| MONO-MAC-6 cell | Growth inhibition assay | Inhibition of human MONO-MAC-6 cell growth in a cell viability assay.IC50=8.27066 μM | ||||
| MZ2-MEL cell | Growth inhibition assay | Inhibition of human MZ2-MEL cell growth in a cell viability assay.IC50=0.28537 μM | ||||
| MPP-89 cell | Growth inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay.IC50=0.04049 μM | ||||
| MZ7-mel cell | Growth inhibition assay | Inhibition of human MZ7-mel cell growth in a cell viability assay.IC50=0.47911 μM | ||||
| LOXIMVI cell | Growth inhibition assay | Inhibition of human LOXIMVI cell growth in a cell viability assay.IC50=0.31503 μM | ||||
| NALM-6 cell | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay.IC50=0.19295 μM | ||||
| NB13 cell | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay.IC50=19.4877 μM | ||||
| NB5 cell | Growth inhibition assay | Inhibition of human NB5 cell growth in a cell viability assay.IC50=1.39827 μM | ||||
| NB17 cell | Growth inhibition assay | Inhibition of human NB17 cell growth in a cell viability assay.IC50=3.63847 μM | ||||
| NCCIT cell | Growth inhibition assay | Inhibition of human NCCIT cell growth in a cell viability assay.IC50=2.86616 μM | ||||
| NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay.IC50=0.14436 μM | ||||
| NCI-H1304 cell | Growth inhibition assay | Inhibition of human NCI-H1304 cell growth in a cell viability assay.IC50=28.1628 μM | ||||
| NCI-H1395 cell | Growth inhibition assay | Inhibition of human NCI-H1395 cell growth in a cell viability assay.IC50=42.0163 μM | ||||
| MHH-PREB-1 cell | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay.IC50=0.74469 μM | ||||
| MLMA cell | Growth inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay.IC50=0.14032 μM | ||||
| MN-60 cell | Growth inhibition assay | Inhibition of human MN-60 cell growth in a cell viability assay.IC50=15.1979 μM | ||||
| MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay.IC50=4.36454 μM | ||||
| NB6 cell | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay.IC50=9.92259 μM | ||||
| NCI-H1355 cell | Growth inhibition assay | Inhibition of human NCI-H1355 cell growth in a cell viability assay.IC50=0.11028 μM | ||||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
Informazioni chimiche, conservazione e stabilità
| Peso molecolare | 506.02 | Formula | C22H28ClN7O3S |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 863127-77-9 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | BMS-354825 Monohydrate | Smiles | CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO.O | ||
Solubilità
|
In vitro |
DMSO
: 100 mg/mL
(197.62 mM)
Water : Insoluble 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 |
Abl
(Cell-free assay) 0.6 nM
Src
(Cell-free assay) 0.8 nM
c-Kit (D816V)
(Cell-free assay) 37 nM
c-Kit (wt)
(Cell-free assay) 79 nM
|
|---|---|
| In vitro |
Dasatinib è più efficace dell'imatinib nell'inibire la proliferazione delle cellule Ba/F3 che esprimono Bcr-Abl wild-type e mutanti di Bcr-Abl, con l'eccezione di T315I. Dasatinib ha una potenza aumentata di due ordini di grandezza (circa 325 volte) rispetto all'imatinib. Dasatinib inibisce potentemente la chinasi Abl wild-type e tutti i mutanti eccetto T315I in un intervallo ristretto. Dasatinib colpisce direttamente i domini chinasi Abl wild-type e mutanti e inibisce l'autofosforilazione e la fosforilazione del substrato in modo concentrazione-dipendente. Dasatinib mostra una potenza 325 volte maggiore rispetto all'imatinib contro le cellule che esprimono Bcr-Abl wild-type. La percentuale di colonie di cellule di midollo osseo TgE diminuisce dal 100% nei pozzetti non trattati al 4,12% nei pozzetti trattati con Dasatinib. In presenza di Dasatinib, la differenza nella percentuale di colonie formate da cellule di midollo osseo WT e TgE è statisticamente significativa. L'espressione di LMP2A è in grado di promuovere la sopravvivenza e la proliferazione dei linfociti B, che può essere inibita prendendo di mira le chinasi Lyn e/o c-Abl tramite Dasatinib. Il trattamento con Dasatinib inibisce la segnalazione di Src, diminuisce la crescita e induce l'arresto del ciclo cellulare e l'apoptosi in un sottogruppo di cellule di carcinoma tiroideo. Il trattamento con dosi crescenti di Dasatinib (da 0,019 μM a 1,25 μM) per 3 giorni inibisce la crescita delle linee cellulari C643, TPC1, BCPAP e SW1736 di circa il 50% a basse concentrazioni nanomolari, mentre sono necessarie concentrazioni più elevate per inibire la crescita della linea cellulare K1. Il trattamento con 10 nM o 50 nM di Dasatinib si traduce in un aumento del 9-22% delle cellule nella popolazione G1 tra le cellule BCPAP, SW1736 e K1, e una corrispondente diminuzione del 7-18% nella percentuale di cellule in fase S.
|
| Saggio chinasico |
Saggi di autofosforilazione della chinasi
|
|
Vengono eseguiti saggi chinasici utilizzando proteine di fusione glutatione S-transferasi (GST)-Abl wild-type e mutanti (amminoacidi 220-498 di c-Abl). Le proteine di fusione GST-Abl vengono rilasciate dalle perle di glutatione-Sepharose prima dell'uso; la concentrazione di ATP è di 5 μM. Immediatamente prima dell'uso nei saggi di autofosforilazione della chinasi e di fosforilazione del substrato peptidico in vitro, le proteine di fusione del dominio chinasico GST-Abl vengono trattate con tirosina fosfatasi LAR. Dopo 1 ora di incubazione a 30 °C, la fosfatasi LAR viene inattivata mediante aggiunta di vanadato di sodio (1 mM). L'analisi immunoblot che confronta la chinasi GST-Abl non trattata con la chinasi GST-Abl defosforilata viene eseguita di routine utilizzando l'anticorpo specifico per la fosfotirosina 4G10 per confermare la defosforilazione completa (>95%) dei residui di tirosina e l'anticorpo c-Abl CST 2862 per confermare il carico uguale della chinasi GST-Abl. L'intervallo di concentrazione di Dasatinib viene esteso a 1.000 nM per il mutante T315I. Le stesse concentrazioni di inibitore vengono utilizzate per i saggi di fosforilazione del substrato peptidico in vitro. I tre inibitori vengono testati negli stessi intervalli di concentrazione contro la chinasi GST-Src e la chinasi GST-Lyn.
|
|
| In vivo |
Dasatinib inverte la splenomegalia nei topi doppiamente transgenici LMP2A/MYC. Dasatinib previene specificamente la formazione di colonie da parte di cellule B del midollo osseo che esprimono LMP2A e riduce le dimensioni della milza nei topi TgE. La massa splenica è significativamente ridotta nei topi Tg6/λ-MYC trattati con Dasatinib rispetto al gruppo di controllo. Dasatinib inibisce la linfoadenopatia nei topi doppiamente transgenici LMP2A/MYC. Dasatinib inverte la splenomegalia nei topi Rag1KO trapiantati con cellule tumorali da topi doppiamente transgenici LMP2A/MYC. La terapia con Dasatinib inibisce la fosforilazione di Lyn nei tumori dei linfociti B che esprimono LMP2A.
|
Riferimenti |
|
Applicazioni
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) p27 / p21 cleaved caspase 3 p-FAK/p-STAT3 |
|
23049975 |
| Growth inhibition assay | Cell viability |
|
23721490 |
| Immunofluorescence | SRC / Met α-tubulin F-actin / Actinin-4 / Paxillin |
|
26517812 |
| ELISA | TNF-α E-selectin VCAM-1 |
|
17684099 |
Informazioni sullo studio clinico
(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT05527418 | Recruiting | Recent HIV-1 Infection |
Eva Bonfill|Institut d''Investigacions Biomèdiques August Pi i Sunyer |
January 26 2024 | Phase 2 |
| NCT05993949 | Recruiting | Lymphoblastic Leukemia |
Stanford University|Kite Pharma |
October 2 2023 | Phase 1 |
| NCT05780073 | Recruiting | HIV Infection Primary |
Fundació Institut Germans Trias i Pujol|Fundación FLS de Lucha Contra el Sida Enfermedades Infecciosas y Promoción de la Salud y Ciencia|Spanish Clinical Research Network - SCReN|IrsiCaixa|University of Turin Italy|Instituto de Salud Carlos III|Germans Trias i Pujol Hospital |
October 16 2023 | Phase 2 |
| NCT05198843 | Terminated | Anatomic Stage IV Breast Cancer AJCC v8|Metastatic Triple-Negative Breast Inflammatory Carcinoma |
National Cancer Institute (NCI) |
November 8 2022 | Phase 1|Phase 2 |
| NCT04925648 | Recruiting | Metastatic Prostate Cancer |
St Vincent''s Hospital Sydney |
October 18 2021 | Phase 2 |
Supporto tecnico
Istruzioni per la manipolazione
Tel: +1-832-582-8158 Ext:3
Per qualsiasi altra domanda, si prega di lasciare un messaggio.
Domande Frequenti
Domanda 1:
What's the difference between S1021 and S7782?
Risposta:
Usually, hydrate will be more stable and dissolve better than free base. But this compound (S1021) dissolves better in DMSO than it (S7782).
I prodotti sono solo per uso di ricerca. Non per uso umano. Non vendiamo a pazienti.
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