BMS-536924

BMS-536924 is a dual inhibitor of insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IC50s = 100 and 73 nM, respectively).{29658} In this way, it blocks IGF-1R 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 IGF-1R and causes growth inhibition and polarization of breast cancer MCF-7 cells.{29655,29657} It also induces expression of cytochrome P450 3A4 isoform in primary hepatocytes.{29656}