CC-115

CC-115 is a dual inhibitor of mammalian target of rapamycin (mTOR) and DNA protein kinase (DNA-PK, IC50s = 0.021 and 0.013 µM, respectively). It is selective for mTOR and DNA-PK over PI3Kalpha, ATM, and ATR (IC50s = 0.85, >30, and >30 µM, respectively). CC-115 inhibits growth in a panel of 123 cancer cell lines, including breast, head and neck, and lung cancer cells (GI50s = 0.015-1.77 µM), and non-homologous end joining (NHEJ) in CAL-51 and MDA-MB-231 breast, PC3 prostate, and HCT116 colon cancer cells (IC50s = 3.15, 2.16, 2.72, and 6.35 µM, respectively). It reduces tumor growth in a PC3 prostate cancer mouse xenograft model when administered at doses of 0.25, 0.5, and 1 mg/kg twice per day.Formal Name: 1-ethyl-3,4-dihydro-7-[2-methyl-6-(1H-1,2,4-triazol-5-yl)-3-pyridinyl]-pyrazino[2,3-b]pyrazin-2(1H)-one. CAS Number: 1228013-15-7. Molecular Formula: C16H16N8O. Formula Weight: 336.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:10): 0.01 mg/ml. lambdamax: 254, 349 nm. SMILES: CCN1C2=NC(C3=C(C)N=C(C4=NN=CN4)C=C3)=CNC2=NCC1=O. InChi Code: InChI=1S/C16H16N8O/c1-3-24-13(25)7-18-15-16(24)22-12(6-17-15)10-4-5-11(21-9(10)2)14-19-8-20-23-14/h4-6,8H,3,7H2,1-2H3,(H,17,18)(H,19,20,23). InChi Key: GMYLVKUGJMYTFB-UHFFFAOYSA-N.