BMS-754807

BMS-754807 is an orally bioavailable antagonist of human insulin-like growth factor type I receptor (IGF-1R) with potential antineoplastic activity. [1] BMS-754807 inhibits the phosphorylation of IGF-1R (IC50 = 13nM) and the downstream targets Akt (IC50 = 22nM) and MAPK (IC50 = 13nM) in the IGF-Sal cell line with IC50 consistent with the antiproliferative IC50 (7 nM) in this cell line. [1] The protein binding for BMS-754807 ranges from of 98.5%in mouse plasma to 95.9%in human plasma. [1]BMS-754807 (Compound 9d) achieved complete tumor growth inhibition at the 6.25 mg/kg dose. This agent was identified with strong efficacy in the IGF-Sal tumor model with minimal weight loss at the upper dose. [1]

BMS-754807 Chemical Structure