CAY10682

(±)-Nutlin-3 (Cay-10004372) blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-kappaB pathway. It specifically prevents phosphorylation of IkappaBalpha by the kinases IKKalpha, IKKbeta, and IKK? (IC50s = 80.5, 78.2, and 57.1 µM, respectively). CAY10682 blocks the growth of cancer cells in vitro (IC50s = 2-6 µM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.Formal Name: 4-(4-bromophenyl)-1-[(4-fluorophenyl)methyl]-4,5-dihydro-5-[3-(1H-imidazol-1-yl)propyl]-3-phenyl-pyrrolo[3,4-c]pyrazol-6(1H)-one. CAS Number: 1542066-74-9. Molecular Formula: C30H25BrFN5O. Formula Weight: 570.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.25 mg/ml, Ethanol: 2 mg/ml. lambdamax: 252 nm. SMILES: O=C1N(CCCN2C=CN=C2)C(C3=CC=C(Br)C=C3)C4=C1N(CC5=CC=C(F)C=C5)N=C4C6=CC=CC=C6. InChi Code: InChI=1S/C30H25BrFN5O/c31-24-11-9-23(10-12-24)28-26-27(22-5-2-1-3-6-22)34-37(19-21-7-13-25(32)14-8-21)29(26)30(38)36(28)17-4-16-35-18-15-33-20-35/h1-3,5-15,18,20,28H,4,16-17,19H2. InChi Key: WBTRUQGSTZSFSK-UHFFFAOYSA-N.