solo per uso di ricerca
Nilotinib (AMN-107) Bcr-Abl inibitore
N. Cat.S1033
Struttura chimica
Peso molecolare: 529.52
Vai a
Controllo Qualità
Lotto:
Purezza:
99.97%
99.97
Coltura cellulare, trattamento e concentrazione di lavoro
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | PMID |
|---|---|---|---|---|---|---|
| EoL-1-cell | Growth Inhibition Assay | IC50=0.000144 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=0.00248 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.0041 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.0049 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.00828 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.01089 μM | SANGER | |||
| KASUMI-1 | Growth Inhibition Assay | IC50=0.02413 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=0.13439 μM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=0.64263 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.6487 μM | SANGER | |||
| HMV-II | Growth Inhibition Assay | IC50=0.74874 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=0.9015 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=1.02228 μM | SANGER | |||
| NCI-H1703 | Growth Inhibition Assay | IC50=1.1887 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=1.27416 μM | SANGER | |||
| ACN | Growth Inhibition Assay | IC50=1.55077 μM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=1.57205 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=1.82077 μM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=2.73793 μM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=2.74327 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=2.87102 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=2.90623 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=2.92084 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=3.01313 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=3.40092 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=3.43029 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=3.61107 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=3.64169 μM | SANGER | |||
| HT-1080 | Growth Inhibition Assay | IC50=3.91775 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=4.31203 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=4.80282 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=4.83191 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=4.88242 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=4.90907 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=5.48938 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=5.77471 μM | SANGER | |||
| RVH-421 | Growth Inhibition Assay | IC50=5.77536 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=5.9036 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=6.31359 μM | SANGER | |||
| MDA-MB-361 | Growth Inhibition Assay | IC50=6.33699 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=6.47191 μM | SANGER | |||
| NY | Growth Inhibition Assay | IC50=6.53599 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=6.66931 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=6.73964 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=7.11953 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=7.28287 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=7.40149 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=7.47155 μM | SANGER | |||
| SK-MEL-24 | Growth Inhibition Assay | IC50=7.63392 μM | SANGER | |||
| COLO-679 | Growth Inhibition Assay | IC50=7.98671 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=8.32054 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=8.38481 μM | SANGER | |||
| UM-UC-3 | Growth Inhibition Assay | IC50=8.43956 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=8.53582 μM | SANGER | |||
| COLO-668 | Growth Inhibition Assay | IC50=8.59491 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=8.62353 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=8.83756 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=8.87128 μM | SANGER | |||
| BCPAP | Growth Inhibition Assay | IC50=9.02562 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=9.09831 μM | SANGER | |||
| ACHN | Growth Inhibition Assay | IC50=9.23632 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=9.33482 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=9.76497 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=10.0132 μM | SANGER | |||
| HEC-1 | Growth Inhibition Assay | IC50=10.2804 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=10.6853 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=10.8923 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=10.9245 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=11.0635 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=11.2101 μM | SANGER | |||
| NCI-N87 | Growth Inhibition Assay | IC50=11.7731 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=11.7953 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=11.8839 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=12.6801 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=12.9307 μM | SANGER | |||
| AGS | Growth Inhibition Assay | IC50=13.0351 μM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=13.0512 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=13.3256 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=13.4102 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=13.4972 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=13.5843 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=13.5856 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=13.8137 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=14.1184 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=14.2656 μM | SANGER | |||
| NCI-H2029 | Growth Inhibition Assay | IC50=14.2727 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=14.6046 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=15.5683 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=16.0241 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=16.3802 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=16.6203 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=17.0582 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=17.6433 μM | SANGER | |||
| HT-29 | Growth Inhibition Assay | IC50=17.7889 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=18.1122 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=18.3172 μM | SANGER | |||
| BT-549 | Growth Inhibition Assay | IC50=18.4092 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=18.5723 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=18.8341 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=19.0458 μM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=19.2475 μM | SANGER | |||
| 769-P | Growth Inhibition Assay | IC50=19.6335 μM | SANGER | |||
| BALL-1 | Growth Inhibition Assay | IC50=19.6775 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=19.8979 μM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=19.9315 μM | SANGER | |||
| NCI-H630 | Growth Inhibition Assay | IC50=19.9378 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=20.3802 μM | SANGER | |||
| KYSE-150 | Growth Inhibition Assay | IC50=20.7047 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=20.7586 μM | SANGER | |||
| HuP-T3 | Growth Inhibition Assay | IC50=21.0852 μM | SANGER | |||
| MFE-280 | Growth Inhibition Assay | IC50=21.5679 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=21.8408 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=22.0478 μM | SANGER | |||
| NCI-H69 | Growth Inhibition Assay | IC50=22.4299 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=22.4965 μM | SANGER | |||
| NCI-H1993 | Growth Inhibition Assay | IC50=22.4971 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=23.2843 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=23.5357 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=23.8472 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=23.9 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=24.2362 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=24.6767 μM | SANGER | |||
| C32 | Growth Inhibition Assay | IC50=24.9576 μM | SANGER | |||
| HTC-C3 | Growth Inhibition Assay | IC50=25.3577 μM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=25.3943 μM | SANGER | |||
| CAL-85-1 | Growth Inhibition Assay | IC50=25.4577 μM | SANGER | |||
| HT-1197 | Growth Inhibition Assay | IC50=25.5319 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=25.7136 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=25.7785 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=25.962 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=26.0312 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=26.0452 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=26.0915 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=26.4114 μM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=26.4243 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=27.1872 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=27.4349 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=27.6255 μM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=27.9617 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=28.2105 μM | SANGER | |||
| NCI-H2009 | Growth Inhibition Assay | IC50=29.1431 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=29.3685 μM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=29.4001 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=29.458 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=29.5505 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=29.6097 μM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=29.6433 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=29.8366 μM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=29.9904 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=30.5716 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=31.0446 μM | SANGER | |||
| HCC1419 | Growth Inhibition Assay | IC50=31.24 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=31.7429 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=31.8358 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=31.9861 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=32.2634 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=32.31 μM | SANGER | |||
| SBC-5 | Growth Inhibition Assay | IC50=32.8511 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=33.4848 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=34.0741 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=34.0752 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=34.3404 μM | SANGER | |||
| HCC70 | Growth Inhibition Assay | IC50=34.9514 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=34.961 μM | SANGER | |||
| NCI-H1666 | Growth Inhibition Assay | IC50=35.8253 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=35.92 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=36.8049 μM | SANGER | |||
| KNS-62 | Growth Inhibition Assay | IC50=36.9438 μM | SANGER | |||
| SK-MEL-30 | Growth Inhibition Assay | IC50=37.8737 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=38.7341 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=38.8653 μM | SANGER | |||
| SW1116 | Growth Inhibition Assay | IC50=39.2805 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=39.3638 μM | SANGER | |||
| RD | Growth Inhibition Assay | IC50=39.5258 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=39.6916 μM | SANGER | |||
| HuO-3N1 | Growth Inhibition Assay | IC50=40.108 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=40.5674 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=40.5932 μM | SANGER | |||
| SK-MEL-28 | Growth Inhibition Assay | IC50=40.6435 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=41.2137 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=41.7354 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=42.0567 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=42.402 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=42.8018 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=43.3698 μM | SANGER | |||
| T-24 | Growth Inhibition Assay | IC50=43.4369 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=43.4517 μM | SANGER | |||
| LU-135 | Growth Inhibition Assay | IC50=44.0923 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=44.8262 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=45.1654 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=45.4315 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=45.8952 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=45.9256 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=46.7257 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=46.9952 μM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=47.3608 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=47.6007 μM | SANGER | |||
| LoVo | Growth Inhibition Assay | IC50=48.1002 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=48.1871 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=48.2348 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=48.6236 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=48.7242 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=49.4605 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=49.7117 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=49.8518 μM | SANGER | |||
| 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 = 0.001 μM. | 26789553 | ||
| 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 = 0.00154 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 = 0.002 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 = 0.003 μM. | 23301703 | ||
| KU812 | Antiproliferative assay | Antiproliferative activity against human KU812 cells, IC50 = 0.0034 μM. | 21376587 | |||
| 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 = 0.00352 μM. | 30137981 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA, IC50 = 0.0037 μM. | 20817538 | |||
| 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 = 0.00371 μM. | 30137981 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0039 μM. | 26814890 | ||
| 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 = 0.004 μM. | 26789553 | ||
| 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 = 0.00482 μM. | 30137981 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA, IC50 = 0.0052 μM. | 20817538 | |||
| 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 = 0.00634 μM. | 23088644 | ||
| K562 | Antiproliferative assay | Antiproliferative activity against human K562 cells, IC50 = 0.0065 μM. | 21376587 | |||
| 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 = 0.00838 μM. | 23088644 | ||
| 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 = 0.00921 μM. | 30137981 | ||
| 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 = 0.0095 μM. | 23301703 | ||
| 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 = 0.0103 μM. | 23088644 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0128 μM. | 23301703 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50 = 0.015 μM. | 23521020 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0158 μM. | 23301703 | ||
| 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 = 0.016 μM. | 26789553 | ||
| 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 = 0.017 μM. | 26789553 | ||
| 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 = 0.0189 μM. | 30137981 | ||
| Ba/F | Function assay | Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells, IC50 = 0.02 μM. | 20817538 | |||
| K562 | Antiproliferative assay | Antiproliferative activity against human K562 cells, IC50 = 0.021 μM. | 20817538 | |||
| 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 = 0.021 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 = 0.021 μM. | 26789553 | ||
| 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 = 0.022 μM. | 23301703 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.022 μM. | 26195136 | ||
| 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 = 0.023 μM. | 26789553 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0242 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells, IC50 = 0.025 μM. | 20817538 | |||
| 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 = 0.025 μM. | 26789553 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0278 μM. | 23301703 | ||
| 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 = 0.028 μM. | 28280261 | ||
| 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 = 0.0296 μM. | 30137981 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0299 μM. | 23301703 | ||
| 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 = 0.0369 μM. | 30137981 | ||
| 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 = 0.0386 μM. | 23088644 | ||
| K562 | Function assay | Inhibition of BCR-ABL1 autophosphorylation in human K562 cells, IC50 = 0.042 μM. | 20817538 | |||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0435 μM. | 23301703 | ||
| 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 = 0.0546 μM. | 26789553 | ||
| 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 = 0.0607 μM. | 23088644 | ||
| 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 = 0.0616 μM. | 30137981 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells, IC50 = 0.062 μM. | 20817538 | |||
| 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 = 0.0652 μM. | 23088644 | ||
| A31 | Function assay | Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA, IC50 = 0.071 μM. | 20817538 | |||
| A31 | Function assay | Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA, IC50 = 0.071 μM. | 20817538 | |||
| 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 = 0.0872 μM. | 23088644 | ||
| 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 = 0.1 μM. | 28280261 | ||
| 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 = 0.12 μM. | 23301703 | ||
| 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 = 0.12 μM. | 23301703 | ||
| 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 = 0.13 μM. | 23301703 | ||
| 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 = 0.132 μM. | 30137981 | ||
| 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 = 0.15 μM. | 23088644 | ||
| 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 = 0.15 μM. | 23301703 | ||
| GIST882 | Antiproliferative assay | Antiproliferative activity against human GIST882 cells, IC50 = 0.151 μM. | 20817538 | |||
| 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 = 0.159 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 = 0.16 μM. | 23301703 | ||
| 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 = 0.17 μM. | 23301703 | ||
| 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 = 0.202 μM. | 26789553 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.2153 μM. | 23301703 | ||
| GIST882 | Function assay | Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA, IC50 = 0.217 μM. | 20817538 | |||
| K562 | Antiproliferative assay | Antiproliferative activity against human imatinib-resistant K562 cells, IC50 = 0.26 μM. | 21376587 | |||
| 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 = 0.292 μM. | 23088644 | ||
| 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 = 0.314 μM. | 23088644 | ||
| 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 = 0.47 μM. | 26789553 | ||
| 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 = 0.473 μM. | 23088644 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA, IC50 = 0.677 μM. | 20817538 | |||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.7024 μM. | 23301703 | ||
| 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 = 0.775 μM. | 23088644 | ||
| M-NFS-60 | Antiproliferative assay | Antiproliferative activity against mouse M-NFS-60 cells, IC50 = 0.838 μM. | 20817538 | |||
| 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 = 0.87 μM. | 26789553 | ||
| 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 = 1 μM. | 23301703 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.093 μM. | 26789553 | ||
| 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 = 1.1 μM. | 26789553 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1.2 μM. | 23301703 | ||
| 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 = 1.3 μM. | 26789553 | ||
| 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 = 1.4 μM. | 23301703 | ||
| 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 = 1.4 μM. | 26789553 | ||
| NCI-H2286 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay, IC50 = 1.8 μM. | 26191369 | ||
| 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 = 1.8 μM. | 28280261 | ||
| 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 = 2.1 μM. | 26789553 | ||
| 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 = 2.262 μM. | 30137981 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2.39 μM. | 23521020 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against apoptosis-resistant, Philadelphia chromosome-positive human K562 cells after 72 hrs by PrestoBlue colorimetric assay, IC50 = 2.4 μM. | 24835982 | ||
| MDA-MB-435S | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50 = 2.66 μM. | 23521020 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay, IC50 = 2.7 μM. | 26814890 | ||
| 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 = 2.9 μM. | 23301703 | ||
| 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 = 3 μM. | 23301703 | ||
| NCI-H23 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50 = 3.05 μM. | 23521020 | ||
| 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 = 3.9 μM. | 26789553 | ||
| 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 = 4.1 μM. | 26789553 | ||
| CHL | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CHL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 4.2 μM. | 26789553 | ||
| CHO | Function assay | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50 = 4.7 μM. | 23812503 | |||
| T47D | Antiproliferative assay | 72 hrs | Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50 = 6.08 μM. | 23521020 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 6.63 μM. | 23521020 | ||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.92 μM. | 23521020 | ||
| BJ | Antiproliferative assay | 72 hrs | Antiproliferative activity against human BJ cells after 72 hrs by PrestoBlue colorimetric assay, IC50 = 12.8 μM. | 24835982 | ||
| NCI-H460 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 14.41 μM. | 23521020 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 15.1 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 = 16 μM. | 23301703 | ||
| 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 = 21.1 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay, IC50 = 40.75 μM. | 23088644 | ||
| BA/F3 | Antitumor assay | 75 mg/kg | 19 days | Antitumor activity against mouse BA/F3 cells expressing wild type Bcr-Abl xenografted in CB17 SCID mouse assessed as median survival time at 75 mg/kg, po administered on day 3 once daily for 19 days relative to control | 19572547 | |
| BA/F3 | Antitumor assay | 75 mg/kg | 19 days | Antitumor activity against mouse BA/F3 cells expressing wild type Bcr-Abl xenografted in CB17 SCID mouse assessed as increase in mouse survival at 75 mg/kg, po administered on day 3 once daily for 19 days relative to control | 19572547 | |
| vascular smooth muscle cells | Antiangiogenic assay | 0.15 uM | 72 hrs | Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of cell growth at 0.15 uM after 72 hrs | 22853993 | |
| vascular smooth muscle cells | Antiangiogenic assay | 10 to 15 uM | 72 hrs | Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of network formation at 10 to 15 uM after 72 hrs | 22853993 | |
| HEK293 | Function assay | 0.1 to 1 uM | 16 hrs | Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting | 26191369 | |
| HEK293 | Function assay | 0.1 to 1 uM | 16 hrs | Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting | 26191369 | |
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | |||
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Informazioni chimiche, conservazione e stabilità
| Peso molecolare | 529.52 | Formula | C28H22F3N7O |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 641571-10-0 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | AMN-107 | Smiles | CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5 | ||
Solubilità
|
In vitro |
DMSO
: 52 mg/mL
(98.2 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
| Caratteristiche |
A selective inhibitor of native and mutant Bcr-Abl.
|
|---|---|
| Targets/IC50/Ki |
Bcr-Abl
(Murine myeloid progenitor cells) <30 nM
|
| In vitro |
Nilotinib inibisce la proliferazione, la migrazione e la formazione di filamenti di actina, così come l'espressione di α-SMA e collagene negli HSC attivati. Questo composto induce l'apoptosi degli HSC, che è correlata a una ridotta espressione di bcl-2, un aumento dell'espressione di p53, la scissione di PARP, così come un aumento dell'espressione di PPARγ e TRAIL-R. Induce anche l'arresto del ciclo cellulare, accompagnato da una maggiore espressione di p27 e una downregulation della ciclina D1. È interessante notare che questa sostanza chimica non solo inibisce l'attivazione di PDGFR, ma anche di TGFRII tramite Src. Inibisce significativamente la fosforilazione di ERK e Akt stimolata da PDGF e TGFβ. Inoltre, le forme fosforilate di Abl attivate da PDGF e TGFβ negli HSC umani sono inibite da questo agente. Questo inibitore sopprime la maggior parte delle mutazioni di Bcr-Abl resistenti all'imatinib, ad eccezione di T315I. Inibisce l'attivazione di ERK1/2 mediata da PDGF-DD, l'attivazione basale e mediata da PDGF-DD di PDGFRβ e Akt, e la proliferazione dello schwannoma. Questo composto è più potente dell'imatinib, esercitando il suo massimo effetto inibitorio a concentrazioni inferiori ai livelli plasmatici minimi allo stato stazionario. Riduce anche significativamente i livelli di espressione dei geni per TGF-β1 e il fattore di crescita derivato dalle piastrine (PDGF). Questo trattamento inibisce anche significativamente la proliferazione dei fibroblasti polmonari indotta da PDGF. Inibisce la proliferazione delle cellule Ba/F3 che esprimono p210- e p190-Bcr-Abl, o delle cellule K562 e Ku-812F con valori di IC50 ≤12 nM.
|
| In vivo |
Nilotinib riduce la deposizione di collagene e l'espressione di α-SMA nella fibrosi indotta da CCl4 e BDL. Questo composto potrebbe indurre gli HSC ad andare in apoptosi, il che è correlato alla downregulation di bcl-2. Attenua l'entità del danno polmonare e della fibrosi. Questa terapia riduce significativamente i livelli di idrossiprolina ai giorni 14 e 21, il che è accompagnato da livelli di espressione diminuiti del fattore di crescita trasformante (TGF)-β1 e di PDGFRβ. Questa sostanza chimica prolunga la sopravvivenza dei topi iniettati con linee cellulari ematopoietiche trasformate da Bcr-Abl o cellule del midollo primario e prolunga la sopravvivenza nei modelli murini di CML resistenti all'imatinib.
|
Riferimenti |
|
Applicazioni
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | p-AMPKα / AMPKα / p-AMPKβ1 / AMPKγ2 / p-LKB1 / LKB1 / CaMKIIβ DNMT1 / DNMT3a / DNMT3b pABL1 / p-NF-κB1 / NF-κB / STAT3 / p-STAT3 / IL-1β / IL-6 / COX2 |
|
23677989 |
| Growth inhibition assay | Cell viability |
|
23677989 |
Informazioni sullo studio clinico
(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT06409936 | Not yet recruiting | CML Chronic Phase|Chronic Myeloid Leukemia Chronic Phase|Chronic Myeloid Leukemia BCR/ABL-Positive|Chronic Myeloid Leukemia |
Gruppo Italiano Malattie EMatologiche dell''Adulto|Fundacion Espanola para la Curacion de la Leucemia Mieloide Cronica |
September 2024 | Phase 2 |
| NCT05185947 | Recruiting | Gynecologic Cancer|Gynecologic Neoplasms|Peritoneal Carcinomatosis|Peritoneal Neoplasms|Ovarian Cancer|Ovarian Neoplasms|Colorectal Cancer|Colorectal Neoplasms|Appendiceal Cancer|Appendiceal Neoplasms |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
October 13 2022 | Phase 2 |
| NCT04326933 | Unknown status | Patients Diagnosed as Chronic Meyloid Leukemia |
Assiut University |
January 1 2020 | -- |
| NCT04002674 | Recruiting | Dementia With Lewy Bodies |
Georgetown University|National Institutes of Health (NIH) |
July 1 2019 | 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:
I would like to use it for in vivo studies in mice, can you give me some suggestions about the in vivo formulation?
Risposta:
For in vivo study, we recommend to use 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 3mg/ml for it.
I prodotti sono solo per uso di ricerca. Non per uso umano. Non vendiamo a pazienti.
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