RO8994

RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM). It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.Formal Name: (2'S,3R,4'S,5'R)-N-[4-(aminocarbonyl)-2-methoxyphenyl]-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-2-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide. CAS Number: 1309684-94-3. Molecular Formula: C31H31Cl2FN4O4. Formula Weight: 613.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12.5 mg/ml, DMSO: 14 mg/ml, Ethanol: 5 mg/ml. lambdamax: 212, 270, 300 nm. SMILES: O=C(NC1=C(OC)C=C(C(N)=O)C=C1)[C@H](N[C@H]2CC(C)(C)C)[C@H](C3=CC=CC(Cl)=C3F)[C@]2(C4=CC=C(Cl)C=C4N5)C5=O. InChi Code: InChI=1S/C31H31Cl2FN4O4/c1-30(2,3)14-23-31(18-10-9-16(32)13-21(18)37-29(31)41)24(17-6-5-7-19(33)25(17)34)26(38-23)28(40)36-20-11-8-15(27(35)39)12-22(20)42-4/h5-13,23-24,26,38H,14H2,1-4H3,(H2,35,39)(H,36,40)(H,37,41)/t23-,24-,26+,31+/m0/s1. InChi Key: MURAVORBGFDSMA-ISKXDESKSA-N.