Rucaparib monocamsylate

Rucaparib monocamsylate (CAS No.: 1859053-21-6) is a synthetic small molecule, a poly(ADP-ribose) polymerase pathway modulator prepared as the camsylate salt with rucaparib as the active ingredient, classified as a PARP inhibitor, and used for discovery research and early-stage drug development exploration related to DNA damage response and oncology; it has high-affinity inhibitory activity against PARP1 (Ki of 1.4 nM), shows activity against PARP2 and PARP3, also displays measurable binding ability to multiple other PARP domains, and has been reported in the literature to inhibit hexose-6-phosphate dehydrogenase H6PD; mechanistically, this compound can inhibit the catalytic activity of PARP involved in base excision repair, thereby increasing reliance on the homologous recombination pathway in models with impaired BRCA pathway function and supporting the “synthetic lethality” research paradigm; in vitro data overall indicate enzymatic inhibition at the nanomolar level and inhibition of cell proliferation at the low micromolar level, with selective sensitivity observed in homologous recombination-deficient backgrounds; in terms of applications, it is commonly used as a reference PARP inhibitor for analysis of DNA repair signaling at the cellular and molecular levels, target validation and mechanism-of-action studies, development of orthogonal and companion assay methods, as well as combination screening and chemical sensitization evaluation with chemical agents that induce replication stress or DNA damage (such as alkylating agent prodrugs), and it may also be used in animal models such as mouse xenografts to explore pharmacodynamic-related biological readouts of PARP pathway intervention; the specific concentration or dose used in experiments usually depends on the study design and objectives; this product is for laboratory research use only and is not intended for human or veterinary use, clinical administration, diagnostic procedures, or any form of ingestion.