產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 1mg 5mg
CAS	1457983-28-6
別名
化學名	8-bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one
分子式	C25H25BrN6O2
分子量	521.41
溶解度	≥ 26.05mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

G-749 is a selective inhibitor of Fms-like tyrosine receptor kinase-3 (FLT3) with IC50 value of 0.4 nM for wild-type FLT31.

G-749 is a synthesized and ATP-competitive inhibitor of wild-type FLT3 with high potency. It inhibited the autophosphorylation of FLT3 with IC50 value of ≤ 8 nM in RS4-11 leukemia cells. It also has inhibitory activity against various FLT3 mutants. In BaF3 cell lines that stably express FLT3-ITD/N676D, -ITD/F691L, -D835Y or -D835Y/N676D, G-749 showed strong potency against autophosphorylation of all tested FLT3 mutants with IC50 of < 10 nM. In MV4-11 and Molm-14 cell lines addicted to FLT3-ITD, G-749 significantly suppressed cell proliferation as well as increased active caspase 3/7 level and cleaved PARP in a dose-dependent manner. Besides that, G-749 showed high potency against p-FLT3, p-ERK1/2 and p-AKT even in high FLT3 ligand milieu1.

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原創(chuàng)作者：上海莼試生物技術有限公司

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