A reversible, orally bioavailable dual inhibitor of IGF-1R and InsR tyrosine kinases (IC₅₀s = 1.8 and 1.7 nM, respectively); inhibits cell proliferation or induces apoptosis in a variety of cancer cells in vitro; inhibits the growth of tumor xenografts in mice.

BMS-754807 is an inhibitor of the insulin receptor (InsR) and IGF-1R that exhibits anticancer chemotherapeutic activity. BMS-754807 enhances the efficacy of other co-administered chemotherapeutics, decreasing levels of activated Akt, increasing cleavage of PARP and caspase 3, and inhibiting…