WYE-354

WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2. It is a much weaker inhibitor of phosphatidylinositol 3-kinase alpha (IC50 = 1,026 nM) and other kinases. WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors.Formal Name: 4-[6-[4-[(methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic acid, methyl ester. CAS Number: 1062169-56-5. Molecular Formula: C24H29N7O5. Formula Weight: 495.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 30 mg/ml, Ethanol: 0.4 mg/ml. lambdamax: 287 nm. SMILES: O=C(OC)NC1=CC=C(C2=NC(N3CCOCC3)=C4C(N(C5CCN(C(OC)=O)CC5)N=C4)=N2)C=C1. InChi Code: InChI=1S/C24H29N7O5/c1-34-23(32)26-17-5-3-16(4-6-17)20-27-21(29-11-13-36-14-12-29)19-15-25-31(22(19)28-20)18-7-9-30(10-8-18)24(33)35-2/h3-6,15,18H,7-14H2,1-2H3,(H,26,32). InChi Key: IMXHGCRIEAKIBU-UHFFFAOYSA-N.