GNE-490

GNE-490 is an inhibitor of PI3K (IC50s = 3.5, 25, 5.2, and 15 nM for PI3Kalpha, PI3Kbeta, PI3Kdelta, and PI3Kgamma, respectively). It is selective for PI3K over mTOR (IC50 = 740 nM) and a panel of 142 kinases at 1 µM. GNE-490 (0.4 µM) reduces cell migration by, the number of vessel outgrowths from, and induces apoptosis in, human umbilical vein endothelial cells (HUVECs). It increases the length of circadian rhythms in zebrafish larvae. GNE-490 (30 mg/kg) decreases vascularization and tumor growth in a PC3 prostate cancer mouse xenograft model.Formal Name: 2-(2-amino-4-methyl-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine-6-methanol. CAS Number: 1033739-92-2. Molecular Formula: C18H22N6O2S. Formula Weight: 386.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml. SMILES: OC(C)(C)C1=CC(N=C(C2=CN=C(N)N=C2C)N=C3N4CCOCC4)=C3S1. InChi Code: InChI=1S/C18H22N6O2S/c1-10-11(9-20-17(19)21-10)15-22-12-8-13(18(2,3)25)27-14(12)16(23-15)24-4-6-26-7-5-24/h8-9,25H,4-7H2,1-3H3,(H2,19,20,21). InChi Key: SFWTVVNNVHWDEE-UHFFFAOYSA-N.