BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM. BMS-794833 also inhibits Ron (Met family), Axl (phylogenetically related Axl/Tyro3/Mer subfamily) and Flt-3 with IC50 values less than 3 nM. The compound was selective versus a panel of greater than 200 additional receptor tyrosine kinase (RTKs), non-RTKs and serine/threonine kinases based on biochemical or Ambit binding assays. Moreover, it inhibited the cell growth in GTL-16 gastric carcinomas with an IC50 of 39 nM . In vivo, BMS-794833 exhibited dose-dependent anti-tumor activity against multiple tumor types without overt toxicities at efficacious dose levels.
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