BMS-754807 is a potent and reversible inhibitor of the insulin-like growth factor 1 receptor/insulin receptor (IGF-1R/IR) family kinases (Ki, <2 nmol/L). BMS-754807 effectively inhibits the growth of a broad range of human tumor types in vitro, including mesenchymal, epithelial, and hematopoietic tumor cell lines (IC₅₀, 5–365 nmol/L).