BAY-8400

BAY-8400 is an inhibitor of DNA-dependent protein kinase (DNA-PK, IC50 = 0. µM). It is selective for DNA-PK over ataxia-telangiectasia mutated kinase (ATM) and mTOR (IC50s = 19. and 1. µM, respectively) and a panel of 365 additional kinases at 1 µM but does inhibit ataxia-telangiectasia and Rad3-related protein/kinase (ATR) and PI3Kbeta (IC50s = 0. and 0. µM, respectively). BAY-8400 inhibits the formation of gammaH2AX in ATM-negative HT-144 melanoma cells (IC50 = 0. nM) and reduces the proliferation of HT-29 colon cancer cells when used alone or in combination with bleomycin. In vivo, BAY-8400 (150 mg/kg, p.o.) reduces tumor area in an LNCaP prostate cancer mouse xenograft model when administered in combination with BAY 2315497. InChI: InChI=1S/C21H17F2N5O/c22-20(23)16-8-15(10-24-11-16)14-3-4-17-18(9-14)28-19(12-25-17)26-27-21(28)13-2-1-6-29-7-5-13/h2-4,8-12,20H,1,5-7H2, InChIKey: ATKHYZXUMVNCIO-UHFFFAOYSA-N, SMILES: FC(F)C1=CN=CC(C2=CC3=C(C=C2)N=CC4=NN=C(C5=CCCOCC5)N34)=C1