SKLB197

SKLB197 is an inhibitor of ataxia-telangiectasia and Rad3-related protein/kinase (ATR) (IC50 = 0.013 µM). It is selective for ATR over a panel of 402 other kinases (IC50s = >1 µM). SKLB197 reduces growth in cancer cell lines deficient in ataxia-telangiectasia mutated kinase (ATM, IC50s = 0.13-0.66 µM) to a greater extent than in ATM-expressing cancer cell lines (IC50s = 3.66-8.79 µM). It induces apoptosis in ATM-deficient LoVo colorectal cancer cells but not in ATM-expressing HT-29 colorectal cancer cells and reduces tumor growth in a LoVo mouse xenograft model when administered at doses of 50 or 100 mg/kg.. SMILES: C[C@H]1N(CCOC1)C2=NC(C3=C4C=CNC4=CC=C3)=NC5=C2C=C(C6=CC=NN6C)C=C5. InChi Code: InChI=1S/C25H24N6O/c1-16-15-32-13-12-31(16)25-20-14-17(23-9-11-27-30(23)2)6-7-22(20)28-24(29-25)19-4-3-5-21-18(19)8-10-26-21/h3-11,14,16,26H,12-13,15H2,1-2H3/t16-/m1/s1. InChi Key: FCNFJRRMUAOHKI-MRXNPFEDSA-N