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

MET:1.7 nM, VEGFR2:15 nM

At a dosage of 25 mg/kg, BMS798433 exhibited complete inhibition of tumor growth in the U87 glioblastoma model. In the GTL-16 human gastric tumor xenograft model, treatment with BMS798433 for 14 days resulted in a Tumor Growth Inhibition (TGI) rate of over 50% within at least one tumor doubling time, with no significant toxicity observed during the period.

BMS794833 inhibits the activation of the Met receptor in the gastric cancer cell line GTL-16, with an IC50 of 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)