PHT-427

PHT-427 is an inhibitor of the serine/threonine kinases Akt and phosphoinositide-dependent protein kinase-1 (PDPK1) with Ki values of 2.7 and 5.2 µM, respectively, that selectively binds to the pleckstrin homology binding domain of both kinases. PHT-427 (10 µM) inhibits PDPK1 and Akt autophosphorylation in BxPC-3 prostate cancer cells. In vivo, PHT-427 (125-250 mg/kg) reduces tumor growth in BxPC-3, Panc-1, MiaPaCa-2, PC3, SKOV3, A549, and MCF-7 xenograft mouse models, with up to 80% reduction in growth for those containing PIK3CA mutations. PHT-427 (200 mg/kg) also enhances the antitumor effect of paclitaxel (Cay-10461) in an MCF-7 breast cancer xenograft mouse model.Formal Name: 4-dodecyl-N-1,3,4-thiadiazol-2-yl-benzenesulfonamide. CAS Number: 1191951-57-1. Synonyms: Akt Inhibitor XIV. Molecular Formula: C20H31N3O2S2. Formula Weight: 409.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.20 mg/ml, DMSO: 16 mg/ml. lambdamax: 226, 270 nm. SMILES: CCCCCCCCCCCCC1=CC=C(S(NC2=NN=CS2)(=O)=O)C=C1. InChi Code: InChI=1S/C20H31N3O2S2/c1-2-3-4-5-6-7-8-9-10-11-12-18-13-15-19(16-14-18)27(24,25)23-20-22-21-17-26-20/h13-17H,2-12H2,1H3,(H,22,23). InChi Key: BYWWNRBKPCPJMG-UHFFFAOYSA-N.