GDC-0032

GDC-0032 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoforms alpha, delta, and gamma (IC50s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kbeta. It is over 1,000-fold selective for p100alpha over other PI3K-like kinases, including DNA-dependent protein kinase catalytic subunits, ATM, and ATR. GDC-0032 has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo, suppressing the growth of tumors in a mouse xenograft model at low drug dose levels.Formal Name: 4-[5,6-dihydro-2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]-alpha,alpha-dimethyl-1H-pyrazole-1-acetamide. CAS Number: 1282512-48-4. Synonyms: Taselisib. Molecular Formula: C24H28N8O2. Formula Weight: 460.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 70 mg/mL, Ethanol: <1 mg/mL, Water: <1 mg/mL. lambdamax: 217, 301, 321 nm. SMILES: CC1=NN(C(C)C)C(C2=CN(CCO3)C(C4=C3C=C(C5=CN(C(C)(C)C(N)=O)N=C5)C=C4)=N2)=N1. InChi Code: InChI=1S/C24H28N8O2/c1-14(2)32-22(27-15(3)29-32)19-13-30-8-9-34-20-10-16(6-7-18(20)21(30)28-19)17-11-26-31(12-17)24(4,5)23(25)33/h6-7,10-14H,8-9H2,1-5H3,(H2,25,33). InChi Key: BEUQXVWXFDOSAQ-UHFFFAOYSA-N.