BMS-536924 is a dual inhibitor of insulin-like growth factor receptor (IGF1R) kinase and insulin receptor (IC50s = 100 and 73 nM, respectively). In this way, it blocks IGF1R autophosphorylation and signaling through MEK1/2 and Akt, leading to G1 arrest and apoptosis in myeloblastic leukemia ML-1 cells. BMS-536924 reverses epithelial-to-mesenchymal transition in immortalized mammary epithelial MCF10A cells overexpressing constitutively activated IGF1R and causes growth inhibition and polarization of breast cancer MCF-7 cells. It also induces expression of cytochrome P450 3A4 isoform in primary hepatocytes.
