PKI-402

PKI-402 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR, IC50s = 1.4, 9.2, and 1.7 nM for PI3Kalpha, PI3Kgamma, and mTOR, respectively). It reduces proliferation of MDA-MB-361 and PC3 cancer cells (IC50s = 8 and 21 nM, respectively) and inhibits phosphorylation of Akt in MDA-MB-361 cells (IC50 = 5 nM). PKI-402 (25, 50, and 100 mg/kg) reduces intratumor phosphorylation of Akt and tumor growth in an MDA-MB-361 mouse xenograft model. It also inhibits tumor growth in U87MG glioma and A549 lung cancer mouse xenograft models in a dose-dependent manner.Formal Name: N-[4-[3-ethyl-7-(4-morpholinyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-yl]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-urea. CAS Number: 1173204-81-3. Molecular Formula: C29H34N10O3. Formula Weight: 570.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: CN1CCN(C(C2=CC=C(NC(NC3=CC=C(C4=NC(N5CCOCC5)=C(N=NN6CC)C6=N4)C=C3)=O)C=C2)=O)CC1. InChi Code: InChI=1S/C29H34N10O3/c1-3-39-27-24(34-35-39)26(37-16-18-42-19-17-37)32-25(33-27)20-4-8-22(9-5-20)30-29(41)31-23-10-6-21(7-11-23)28(40)38-14-12-36(2)13-15-38/h4-11H,3,12-19H2,1-2H3,(H2,30,31,41). InChi Key: ZAXFYGBKZSQBIV-UHFFFAOYSA-N.