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编 号:F753425
分子式:C20H25F3N6O
分子量:422.45
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生物活性:
FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase?inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM).

体内研究:
Oral administration of FLT3-IN-11 (compound 30) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5%.

体外研究:
FLT3-IN-11 (compound 30) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y.
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