BMS-536924

BMS-536924 is a potent small molecule dual IGF-IR/IR kinase inhibitor, which shows antitumor activity in multiple tumor models. BMS-536924 inhibits cellular proliferation and disrupts Akt and MAPK phosphorylation. BMS-536924 also inhibits FAK and Lck with IC50 of 150 nM and 341 nM, respectively. BMS-536924 induced a dose-dependent inhibition of proliferation, with an accumulation of cells in G(0)/G(1,), and completely blocked CD8-IGF-IR-induced migration, invasion, and anchorage-independent growth in monolayer culture. In vitro, BMS-536924 inhibited leukemic colony formation in CD34+ clinical AML samples.