BMS-777607 is an orally available, ATP-competitive Met kinase inhibitor with IC50 of 3.9 nM with additional activity against related kinases such as Axl and Ron at 1.1 nM, and 1.8 nM, respectively [1] BMS-777607 blocks autophosphorylation of c-Met at and IC50 of 20 nM and also blocks downstream activation of Akt and extracellular signal-regulated kinases. [2]

Because of its added ability to suppress HGF-stimulated cell migration and invasion in a dose-dependent fashion (IC50 < 100 nM), BMS-777607 is being considered as a potential for the treatment of advanced prostate cancer. [2]

Additional studies have shown that BMS-777607 suppressed c-Met-associated cellular funcdtions in PC-3 cells expressing constitutively activated c-Met; these findings suggest the possibility that in cancers where hyperactive c-Met is independent of HGF-mediated autocrine stimulation, targeting Met may be more effective than targeting the HGF ligand to impede cancer progression and metastasis. [3]