Potent and selective ATM kinase inhibitor (IC50 = 0.6 nM in an enzyme inhibition assay). Exhibits > 600-fold selectivity for ATM over other kinases. Inhibits ATM kinase in an in vitro cellular assay (IC50 = 0.33 μM). Potentiates the antitumor effects of the topoisomerase 1 inhibitor irinotecan in tumor bearing, immunocompromised mice. Orally bioavailable. Degorce et al (2016) Discovery of novel 3-quinoline carboxamides as potent, selective and orally bioavailable inhibitors of ataxiatelangiectasiamutated (ATM) kinase. J.Med.Chem. 59 6281 PMID:27259031
Antitumor agent-28 is a compound that specifically targets and inhibits the activity of the ataxiatelangiectasiamutated (ATM) kinase. By doing so, it effectively impedes the progression of ATM-mediated diseases and demonstrates significant anti-cancer activity.
ATR-IN-4, a potent inhibitor of ATR (Ataxiatelangiectasiamutated gene Rad 3-associated kinase), restricts the growth of DU145 prostate cancer cells and NCI-H460 lung cancer cells, with IC 50 values of 130.9 nM and 41.33 nM, respectively.