BMS794833 是一种 VEGFR2 和 Met 的抑制剂，它们的IC50值分别为 15 和 1.7 nM。摘自专利WO2009094417， 化合物实例1，

BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2; a prodrug of BMS-817378.

BMS798433在25 mg/kg的剂量下对U87胶质母细胞瘤模型也显示完全抑制肿瘤生长作用.在GTL-16人胃肿瘤异种移植模型中,BMS798433处理14天,在至少一个肿瘤倍增时间内显示大于50％的TGI,期间没有观察到明显的毒性.

BMS794833抑制Met受体激活的胃癌细胞系GTL-16,IC50 为39 nM。

Met kinase assay: BMS798433 is dissolved in DMSO and diluted by water before use. The reaction solution contains baculovirus expressed GST-Met kinase, 20 mM Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1 mg BSA, 0.1 mg polyGlu4/tyr, 1 μM ATP and 0.2μCi γ–ATP. Reactions are incubated at 30 °C for 1 hour and stopped by 8% TCA. TCA precipitates are collected onto GF/C plates using a universal harvester and the filters are quantitated using liquid scintillation counter.

GTL-16 cells are seeded into 96 well plates and incubated for 24 hours. BMS798433 is dissolved in DMSO at 10 mM and diluted with culture medium before use. Then BMS798433 is added to the cells for 72 hours. After that, MTS assay is used to measure the IC50.(Only for Reference)

1174046-72-0

C23H15ClF2N4O3

468.84

H2O:<1 mgml
Ethanol:<1 mgml
DMSO:87 mg/mL (185.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years