BMS-536924

BMS-536924 is a potent, small-molecule, ATP-competitive dual inhibitor of the Insulin-like Growth Factor 1 Receptor (IGF-1R) and the Insulin Receptor (IR). Developed by Bristol Myers Squibb, it exhibits high selectivity for these receptors over other tyrosine kinases. By blocking the autophosphorylation of IGF-1R and IR, BMS-536924 inhibits downstream signaling through the PI3K/Akt and MAPK pathways, leading to decreased cell proliferation and increased apoptosis in various tumor models. While it has shown significant preclinical activity in cancers such as ovarian, breast, and lung cancer, and has been studied for its ability to sensitize cells to other agents like PARP inhibitors, it has primarily served as a research tool and did not progress into late-stage clinical development.