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G-749
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
G-749图片
CAS NO:1457983-28-6
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议

产品介绍
G-749 是一种有效的口服活性和 ATP 竞争性 FLT3 抑制剂，对 FLT3 野生型和 FLT3-D835Y 的 IC50 分别为 0.4 nM 和 0.6 nM。 G-749可用于急性髓系白血病（AML）的耐药性研究。
Cas No.1457983-28-6
化学名8-bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one
Canonical SMILESO=C1NC=C(Br)C2=C1C(NC3=CC=C(OC4=CC=CC=C4)C=C3)=NC(NC5CCN(C)CC5)=N2
分子式C25H25BrN6O2
分子量521.41
溶解度≥ 26.05mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

References:
1. Lee H K, Kim H W, Lee I Y, et al. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood, 2014, 123(14): 2209-2219.