产品
编 号：F753426
分子式：C21H23F3N6O
分子量：432.44
分子式：C21H23F3N6O
分子量：432.44
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CAS No: 2499966-67-3
产品详情
生物活性：
FLT3-IN-12 is a potent, selective and orally active FLT3 kinase?inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM).
体内研究：
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.FLT3-IN-12 (compound 36; 20 mg/kg; oral administration) exhibits excellent plasma exposure (area under the curve (AUC)0–∞ of 5278 ng·h/mL), T1/2 of 3.7 hours, and high maximum plasma concentrations (Cmax of 775 ng/mL).
体外研究：
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 IC50 range is 0.16-14.5 nM.
FLT3-IN-12 is a potent, selective and orally active FLT3 kinase?inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM).
体内研究：
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.FLT3-IN-12 (compound 36; 20 mg/kg; oral administration) exhibits excellent plasma exposure (area under the curve (AUC)0–∞ of 5278 ng·h/mL), T1/2 of 3.7 hours, and high maximum plasma concentrations (Cmax of 775 ng/mL).
体外研究：
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 IC50 range is 0.16-14.5 nM.
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