GDC-0980

GDC-0980 is a potent inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms, with IC50 values of 5, 27, 7, and 14 nM for PI3Kalpha, beta, delta, and gamma, respectively, in cell-free assays. It also inhibits mTOR (Ki = 17 nM) but is inactive against a large panel of additional kinases. GDC-0980 induces cell cycle arrest or apoptosis in a range of cancer cell lines. It is effective in vivo, suppressing the growth of a number of tumor xenografts in mice and enhancing the antitumor activity of docetaxel (Cay-11637) in mice.Formal Name: (2S)-1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-2-hydroxy-1-propanone. CAS Number: 1032754-93-0. Synonyms: Apitolisib, RG7422. Molecular Formula: C23H30N8O3S. Formula Weight: 498.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS (pH 7.2)(1:5): 0.15 mg/ml. lambdamax: 205, 271 nm. SMILES: O=C([C@@H](O)C)N(CC1)CCN1CC(S2)=C(C)C3=C2C(N4CCOCC4)=NC(C5=CN=C(N)N=C5)=N3. InChi Code: InChI=1S/C23H30N8O3S/c1-14-17(13-29-3-5-31(6-4-29)22(33)15(2)32)35-19-18(14)27-20(16-11-25-23(24)26-12-16)28-21(19)30-7-9-34-10-8-30/h11-12,15,32H,3-10,13H2,1-2H3,(H2,24,25,26)/t15-/m0/s1. InChi Key: YOVVNQKCSKSHKT-HNNXBMFYSA-N.