RG7388

RG7388 is a non-imidazoline, selective MDM2 inhibitor that blocks the binding of MDM2 to p53 (IC50 = 30 nM). By inhibiting MDM2, RG7388 activates the p53 pathway in SJSA1 osteosarcoma cells and inhibits the growth of xenografts in nude mice. RG7388 is orally available and prolonged daily administration results in loss of MDM2 and p21 protein, growth inhibition, and apoptosis in SJSA1 xenograft tumors. Like other MDM2 inhibitors, RG7388 competitively inhibits multi-drug resistance protein 1 (MRP1) and reverse MRP1-mediated multidrug resistance in cancer cells in a p53-independent manner.Formal Name: 4-[[[(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxy-benzoic acid. CAS Number: 1229705-06-9. Synonyms: Idasanutlin, Ro 5503781. Molecular Formula: C31H29Cl2F2N3O4. Formula Weight: 616.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 100 mg/ml, Ethanol: 8 mg/ml, Water: < 1 mg/ml. lambdamax: 220, 274, 302 nm. SMILES: O=C(NC1=C(OC)C=C(C(O)=O)C=C1)[C@@H]2N[C@@H](CC(C)(C)C)[C@@](C3=C(F)C=C(Cl)C=C3)(C#N)[C@H]2C4=CC=CC(Cl)=C4F. InChi Code: InChI=1S/C31H29Cl2F2N3O4/c1-30(2,3)14-24-31(15-36,19-10-9-17(32)13-21(19)34)25(18-6-5-7-20(33)26(18)35)27(38-24)28(39)37-22-11-8-16(29(40)41)12-23(22)42-4/h5-13,24-25,27,38H,14H2,1-4H3,(H,37,39)(H,40,41)/t24-,25-,27+,31?/m0/s1. InChi Key: TVTXCJFHQKSQQM-LZQLXLIZSA-N.