FLT3 inhibitor 17

Chemical Structure : FLT3 inhibitor 17

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货号: PC-21367Not For Human Use, Lab Use Only.

FLT3 inhibitor 17 is a potent, highly selective FLT3 inhibitor with IC50 of 1.2 nM and 1.4 nM for FLT3 WT and FLT3-D835Y, shows low activity against VEGFR, FGFR, PDGFR, c-KIT, and RET.

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生物&药学活性

FLT3 inhibitor 17 is a potent, highly selective FLT3 inhibitor with IC50 of 1.2 nM and 1.4 nM for FLT3 WT and FLT3-D835Y, shows low activity against VEGFR, FGFR, PDGFR, c-KIT, and RET.
FLT3 inhibitor 17 inhibits FLT3 WT, FLT3-ITD and FLT3 D835Y with IC50 of ~1 nM, weakly inhibits c-KIT and RET with IC50 of 837 nM and 18000 nM.
FLT3 inhibitor 17 shows very limited activity against cardiovascular kinases FGFR1/2 and PDGFRα/β, with IC50 values >2690 nM, also displays minimal inhibition of over 180 other kinases.
FLT3 inhibitor 17 exhibits antiproliferative effects on Molm14cell lines containing mutated FLT3:Molm-14 (FLT3-ITD), Molm-14 (FLT3-ITD/D835Y) and Molm-14 (FLT3-ITD/F691L) with GI50 values of 2-23 nM, reduces the levels of phosphorylated FLT3 in Molm-14 cells.

物理化学性质&存储条件

分子量	374.45
分子式	C21H22N6O
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	(2S,6R)-4-(3-(4-(1H-pyrazol-4-yl)phenyl)imidazo[1,2-b]pyridazin-6-yl)-2,6-dimethylmorpholine

参考文献

1. Sintim HO, et al. ChemMedChem. 2023 Nov 16:e202300442.