Elimusertib

Elimusertib (CAS No.: 1876467-74-1) is a synthetic and highly selective small-molecule inhibitor of the ATR serine/threonine kinase, classified as a research tool molecule for DNA damage response and replication stress signaling pathways, intended for biomedical research and early-stage drug discovery applications such as cancer biology, DNA repair, and synthetic lethality mechanisms. By inhibiting ATR catalytic activity and downregulating downstream checkpoint signaling, it characteristically weakens CHK1 phosphorylation, disrupts S-phase and G2/M-phase cell cycle control, and reduces replication fork stability under endogenous or induced stress conditions; it shows clear selectivity compared with related PIKK family members such as ATM and DNA-PK. In biochemical and cellular systems, it typically exhibits low-nanomolar ATR enzymatic inhibition and produces antiproliferative effects in the nanomolar to submicromolar range in multiple tumor-derived cell models, consistent with its selective targeting of ATR; in models with elevated replication stress or defects in complementary DNA repair pathways, it can show robust single-agent activity and demonstrates significant combination potential with DNA damage-related research approaches, including platinum compounds, PARP pathway inhibitors, ionizing radiation, and targeted alpha-emitting strategies represented by radium-223, thereby supporting the analysis of synthetic lethality mechanisms and sequence-dependent pharmacology. Typical research uses include mechanism-of-action elucidation, pathway validation, combination matrix screening, and effect modeling in cellular and xenograft models; the concentrations or doses used in experiments usually depend on the specific experimental design and research objectives. This material is for laboratory research use only (such as ATR signaling, checkpoint control, and replication stress biology) and is not intended for medical or diagnostic use in humans or animals, or for any form of ingestion.