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). 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. It also induces expression of cytochrome P450 3A4 isoform in primary hepatocytes.Formal Name: 4-[[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone. CAS Number: 468740-43-4. Molecular Formula: C25H26ClN5O3. Formula Weight: 480.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12 mg/ml, DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml, DMSO: 10 mg/ml. lambdamax: 217, 239, 355 nm. SMILES: CC1=C2C(N=C(C3=C(NC[C@@H](O)C4=CC=CC(Cl)=C4)C=CNC3=O)N2)=CC(N5CCOCC5)=C1. InChi Code: InChI=1S/C25H26ClN5O3/c1-15-11-18(31-7-9-34-10-8-31)13-20-23(15)30-24(29-20)22-19(5-6-27-25(22)33)28-14-21(32)16-3-2-4-17(26)12-16/h2-6,11-13,21,32H,7-10,14H2,1H3,(H,29,30)(H2,27,28,33)/t21-/m1/s1. InChi Key: ZWVZORIKUNOTCS-OAQYLSRUSA-N.