berzosertib

Berzosertib is a highly potent and selective, first-in-class small molecule inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase, with lower potency against ATM serine/threonine kinase. ATR is a key regulator of the DNA damage response pathway, particularly in response to replication stress and DNA double-strand breaks. By inhibiting ATR activity, berzosertib disrupts the ATR-checkpoint kinase 1 (Chk1) signaling pathway, preventing activation of DNA damage checkpoints and repair mechanisms. This leads to accumulation of unrepaired DNA damage in rapidly dividing tumor cells, resulting in cell cycle arrest and apoptosis. Berzosertib has shown promising antitumor activity as both monotherapy and in combination with chemotherapy or radiotherapy across several cancer types including ovarian cancer, small cell lung cancer (SCLC), urothelial cancer, prostate cancer, head and neck squamous cell carcinoma (HNSCC), and advanced solid tumors. It was originally invented by Vertex Pharmaceuticals and later licensed to Merck KGaA for further development[1][2][4][5][6][7].

Other names

1232416-25-9Berzosertib [USAN]5-(4-(isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amineMFCD27976794MFCD-27976794MFCD 27976794L423PRV3V3L-423PRV3V3L 423PRV3V3