SU 11274

A specific, ATP-competitive small molecule inhibitor of the catalytic activity of Met. Displays selectivity for Met enzyme versus a panel of other tyrosine kinases with the following IC₅₀ values: Met = 0.02 μM, Flk = 1.3 μM, EGFR = >100 μM, PDGFßR = >20 μM, Tie2 = >100 μM, c-src = >10 μM, cdk2 = >10 μM, and FGFR-1 = 9.7 μM). Inhibition of the Met kinase activity by SU11274 leads to time- and dose-dependent reduced cell growth and induced G1 cell cycle arrest and apoptosis.