GNE-493

GNE-493 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR, IC50s = 3.4, 12, 16, 16, and 32 nM for PI3Kalpha, PI3Kbeta, PI3Kdelta, PI3Kgamma, and mTOR, respectively). It inhibits proliferation of PC3 and MCF-7.1 cells with IC50 values of 330 and 180 nM, respectively. GNE-493 (10 mg/kg per day) reduces tumor volume in PC3 and MCF-7.1 mouse xenograft models, which are PTEN negative or PI3Kalpha activating mutation positive, respectively. It also decreases relative levels of phosphorylated Akt, PRAS40, and S6RP in tumor tissue in the MCF-7.1 mouse xenograft model.Formal Name: 2-(2-amino-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine-6-methanol. CAS Number: 1033735-94-2. Molecular Formula: C17H20N6O2S. Formula Weight: 372.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 16 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 271 nm. SMILES: NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C=C(C(C)(O)C)S4)=N2)C=N1. InChi Code: InChI=1S/C17H20N6O2S/c1-17(2,24)12-7-11-13(26-12)15(23-3-5-25-6-4-23)22-14(21-11)10-8-19-16(18)20-9-10/h7-9,24H,3-6H2,1-2H3,(H2,18,19,20). InChi Key: LEXMMFPAPDGYGZ-UHFFFAOYSA-N.