CAS NO: | 2499966-67-3 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | FLT3-IN-12 is a potent, selective and orally activeFLT3kinase inhibitor withIC50s of 1.48 nM and 2.87 nM forFLT3-WTandFLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity overc-KIT(>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11,IC50of 0.75 nM)[1]. |
IC50& Target | IC50: 1.48 nM (FLT3-WT) and 2.87 nM (FLT3-D835Y)[1] |
体外研究 (In Vitro) | FLT3-IN-12 (compound 36) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y with the IC50range is 0.16-14.5 nM[1]. |
体内研究 (In Vivo) | Oral administration of FLT3-IN-12 (compound 36) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting a tumor growth inhibitory rate of 95.1%. Importantly, FLT3-IN-12 could prolong the mouse survival time in the FLT3-ITD-TKD dual mutation syngeneic mouse model (BaF3-FLT3-ITD-D835Y) at a dose of 6 mg/kg p.o. bid/4W[1]. |
分子量 | 432.44 |
Formula | C21H23F3N6O |
CAS 号 | 2499966-67-3 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |