AMG 232

AMG 232 is an inhibitor of the murine double minute 2 (MDM2) interaction with the tumor suppressor p53 (KD = 0.045 nM, IC50 = 0.6 nM in a cell-free binding assay). It inhibits proliferation of HCT116 p53 wild-type, but not p53-/-, cells (IC50s = 10 nM and >25 µM, respectively). It reduces tumor growth in an SJSA-1 osteosarcoma mouse xenograft model (ED50 = 9.1 mg/kg) and induces complete regression of tumors in the same model when administered at a dose of 75 mg/kg per day for 10 days. It induces apoptosis of SJSA-1 mouse xenograft tumor cells, decreasing BrdU-labeled cells, increasing cleaved caspase-3, and halting the cell cycle.Formal Name: (3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-1-[(1S)-2-methyl-1-[[(1-methylethyl)sulfonyl]methyl]propyl]-2-oxo-3-piperidineacetic acid. CAS Number: 1352066-68-2. Molecular Formula: C28H35Cl2NO5S. Formula Weight: 568.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml. SMILES: O=C1N([C@@H](C(C)C)CS(C(C)C)(=O)=O)[C@H](C2=CC=C(Cl)C=C2)[C@@H](C3=CC(Cl)=CC=C3)C[C@]1(C)CC(O)=O. InChi Code: InChI=1S/C28H35Cl2NO5S/c1-17(2)24(16-37(35,36)18(3)4)31-26(19-9-11-21(29)12-10-19)23(20-7-6-8-22(30)13-20)14-28(5,27(31)34)15-25(32)33/h6-13,17-18,23-24,26H,14-16H2,1-5H3,(H,32,33)/t23-,24-,26-,28-/m1/s1. InChi Key: DRLCSJFKKILATL-YWCVFVGNSA-N.