PRI-724

PRI-724 is a prodrug form of the beta-catenin/CREB-binding protein (CBP) inhibitor C-82 and a derivative of ICG-001 (Cay-16257). It is cytotoxic to GES-1 gastric mucosal and HGC-27, MKN45, and AGS gastric cancer cells (IC50s = 16.53, 9.8, 44.28, and 3.48 µM, respectively) and enhances decreases in viability induced by lonidamine (Cay-14640) or 2-deoxy-D-glucose (2-DG, Cay-14325) in CAL 27, SCC-25, and BICR 22 tongue squamous carcinoma cells. PRI-724 (0.4 mg/animal) reduces hepatic fibrosis in a mouse model of liver fibrosis induced by carbon tetrachloride (CCl4). It reduces the proliferation of CD4+ or CD8+ stem cell memory and central memory T cells in a rhesus macaque model of antiretroviral therapy-suppressed simian immunodeficiency virus (SIV) infection when administered at doses of 10 or 20 mg/kg per day.Formal Name: (6S,9S,9aS)-hexahydro-2,9-dimethyl-4,7-dioxo-N-(phenylmethyl)-6-[[4-(phosphonooxy)phenyl]methyl]-8-(8-quinolinylmethyl)-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide. CAS Number: 1422253-38-0. Molecular Formula: C33H35N6O7P. Formula Weight: 658.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml. SMILES: [H][C@]1(N(C(NCC2=CC=CC=C2)=O)N(C)CC(N1[C@H]3CC4=CC=C(OP(O)(O)=O)C=C4)=O)[C@H](C)N(CC5=CC=CC6=C5N=CC=C6)C3=O. InChi Code: InChI=1S/C33H35N6O7P/c1-22-31-38(29(40)21-36(2)39(31)33(42)35-19-24-8-4-3-5-9-24)28(18-23-13-15-27(16-14-23)46-47(43,44)45)32(41)37(22)20-26-11-6-10-25-12-7-17-34-30(25)26/h3-17,22,28,31H,18-21H2,1-2H3,(H,35,42)(H2,43,44,45)/t22-,28-,31-/m0/s1. InChi Key: VHOZWHQPEJGPCC-AZXNYEMZSA-N.