c-MET inhibitor 7 is a potent, highly selective c-MET inhibitor with IC50 of 0.90 and 0.09 μM for wild-type and D1228V c-MET, respectively.
c-MET inhibitor 7 binds to the hinge region via its indazole group and extending into the back pocket, with significant rearrangement of the back pocket and αC helix residues.
c-MET inhibitor 7 is highly selective, inhibit justs 3 kinases out of a panel of 140 to any significant degree (i.e. >70%).
c-MET inhibitor 7 inhibits D1228V c-MET activity in a cellular system using a homogenous time-resolved FRET target-engagement assay with IC50 of 12 uM.
