NVP-CGM097

NVP-CGM097 is an inhibitor of the protein-protein interaction between murine double minute 2 (MDM2) and p53 (IC50 = 1.7 nM for human MDM2 in a TR-FRET assay). It is selective for human MDM2 (Ki = 1.3 nM) over dog, mouse, and rat Mdm2 (Kis = 20.5, 65.9, and 47.4 nM, respectively). NVP-CGM097 selectively inhibits proliferation of acute myeloid leukemia (AML) cells expressing wild-type p53 (IC50s = 50-1,000 nM) over AML cells expressing mutant p53 (IC50s = >1,000 nM). It induces tumor regression in a patient-derived xenograft (PDX) mouse model of AML when administered at a dose of 100 mg/kg per day.Formal Name: (1S)-1-(4-chlorophenyl)-1,4-dihydro-6-methoxy-7-(1-methylethoxy)-2-[4-[methyl[[trans-4-(4-methyl-3-oxo-1-piperazinyl)cyclohexyl]methyl]amino]phenyl]-3(2H)-isoquinolinone. CAS Number: 1313363-54-0. Molecular Formula: C38H47ClN4O4. Formula Weight: 659.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 25 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 267 nm. SMILES: CN1CCN([C@H]2CC[C@H](CN(C)C3=CC=C(N4[C@@H](C5=CC=C(Cl)C=C5)C6=CC(OC(C)C)=C(OC)C=C6CC4=O)C=C3)CC2)CC1=O. InChi Code: InChI=1S/C38H47ClN4O4/c1-25(2)47-35-22-33-28(20-34(35)46-5)21-36(44)43(38(33)27-8-10-29(39)11-9-27)32-16-14-30(15-17-32)41(4)23-26-6-12-31(13-7-26)42-19-18-40(3)37(45)24-42/h8-11,14-17,20,22,25-26,31,38H,6-7,12-13,18-19,21,23-24H2,1-5H3/t26-,31-,38-/m0/s1. InChi Key: CLRSLRWKONPSRQ-IIPSPAQQSA-N.