LT-540-717

Chemical Structure : LT-540-717

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货号: PC-25801Not For Human Use, Lab Use Only.

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生物&药学活性

LT-540-717 is a potent, selective and orally available FLT3 inhibitor with IC50 of 0.62 nM, inhibits FLT3 mutations FLT3 (ITD), FLT3 (D835V), FLT3 (ITD, D835V), FLT3 (ITD, F69L) with IC50 of 18.22, 1.54, 0.58 and 1.61 nM, respectively.
LT-540-717 displays <100-fold selectivity over CDK4/cycD3, CDK6/CycD1 and CDK7/CycH/MAT1, exhibits little inhibitory activity against other kinases.
LT-540-717 shows the strongest proliferation-inhibition efficacy against MV4-11 cells with IC50 of 0.02 uM.
LT-540-717 shows much more potent anti-proliferative activities against cell lines containing FLT3 (ITD) mutant (MV4-11 and MOLM-13) than cell lines containing wild-type FLT3 or expressing FLT3.
LT-540-717 (25 mg/kg, QD and 50 mg/kg, QD) exhibited antitumor efficacy in MV4-11 xenograft model.

物理化学性质&存储条件

分子量	456.51
分子式	C24H24N8O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-((6-Phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide

参考文献

1. Yanle Zhi, et al. Eur J Med Chem. 2023 Aug 5:256:115448.

LT-540-717

生物&药学活性

物理化学性质&存储条件

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LT-540-717

生物&药学活性

物理化学性质&存储条件

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