azd6738

Ceralasertib (AZD6738) 是一种 ATR 激酶抑制剂 (IC50=1 nM)，具有选择性和口服活性。Ceralasertib 具有抗肿瘤活性。

(S)-Ceralasertib is a potent and selective inhibitor of sulfoximine morpholinopyrimidine ATR with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics. .

Ceralasertib is an orally available inhibitor of ataxia telangiectasia 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-

ICT10336 是一种ATR抑制剂 AZD6738的缺氧反应性前药，具有缺氧特异性。ICT10336 仅在缺氧条件下于体外被激活，并特异性释放 AZD6738，从而抑制ATR的 T1989 和 S428 位点的磷酸化活化。此过程可消除由 HIF1a 介导的缺氧癌细胞适应，进而选择性诱导 2D 和 3D 癌症模型中细胞的死亡。ICT10336 是 CYPOR 活性的代谢底物。

PROTACVHL-type degrader-1 是一种VHL型PROTAC降解剂，可诱导ATM降解，并增强ATR抑制剂AZD6738的效力。