Ceralasertib is an orally available inhibitor of ataxiatelangiectasia and rad3 related (ATR) kinase. Ceralasertib selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine threonine protein kinase CHK1. This prevents ATR-
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 ataxiatelangiectasia mutated (ATM) kinase. J.Med.Chem. 59 6281 PMID:27259031
Antitumor agent-28 is a compound that specifically targets and inhibits the activity of the ataxiatelangiectasia mutated (ATM) kinase. By doing so, it effectively impedes the progression of ATM-mediated diseases and demonstrates significant anti-cancer activity.
ATR-IN-9 is a highly effective inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR). With an IC50 value as low as 10 nM, ATR-IN-9 demonstrates exceptional potency.
ATR-IN-4, a potent inhibitor of ATR (Ataxiatelangiectasia mutated 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.