GNE-477

GNE-477 is a dual inhibitor of PI3K (IC50 = 4 nM for PI3Kalpha) and mTOR (apparent Ki = 21 nM). It inhibits proliferation of MCF-7.1 cells with an EC50 value of 143 nM. It reduces tumor growth in a PC3-NCI tumor xenograft model when administered at doses ranging from 1 to 20 mg/kg per day.Formal Name: 5-[7-methyl-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-2-pyrimidinamine. CAS Number: 1032754-81-6. Molecular Formula: C21H28N8O3S2. Formula Weight: 504.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: NC1=NC=C(C=N1)C2=NC(N3CCOCC3)=C(SC(CN4CCN(S(C)(=O)=O)CC4)=C5C)C5=N2. InChi Code: InChI=1S/C21H28N8O3S2/c1-14-16(13-27-3-5-29(6-4-27)34(2,30)31)33-18-17(14)25-19(15-11-23-21(22)24-12-15)26-20(18)28-7-9-32-10-8-28/h11-12H,3-10,13H2,1-2H3,(H2,22,23,24). InChi Key: AKKCGLXULFRAET-UHFFFAOYSA-N.