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Ceralasertib, also known as AZD6738, is an orally available morpholino-pyrimidine-based inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor Ceralasertib selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis.

Ceralasertib formate is a potent, selective and orally active ATR inhibitor with an IC50 value of 1 nM. Ceralasertib formate inhibits cell viability and induces DNA damage. Ceralasertib formate induces cell senescence. Ceralasertib formate shows antitumor activity[1][2].

[1] Vendetti FP, et al. The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of cisplatin to resolve ATM-deficient non-small cell lung cancer in vivo. Oncotarget. 2015 Dec 29;6(42):44289-305. DOI:10.18632/oncotarget.6247
[2] Kim HJ, et al. Anti-tumor activity of the ATR inhibitor AZD6738 in HER2 positive breast cancer cells. Int J Cancer. 2017 Jan 1;140(1):109-119. DOI:10.1002/ijc.30373