Talazoparib,又称他拉唑帕利,是可口服PARP1/2抑制剂,Ki值分别为1.2和0.9 nM,有抗肿瘤活性。Talazoparib抑制PARP介导的通过碱基切除修复途径的单链DNA断裂修复,增加DNA链断裂积累,导致基因组不稳定性,进而导致细胞凋亡。
参考文献
[1] Wang B, Chu D, Feng Y, et al. Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent. J Med Chem. 2016 Jan 14;59(1):335-57. doi: 10.1021/acs.jmedchem.5b01498(IF:6.054).
[2] Shen Y, Rehman FL, Feng Y, et, al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res. 2013 Sep 15;19(18):5003-15. doi: 10.1158/1078-0432.CCR-13-1391(IF:8.911).
-25~-15℃保存,有效期3年。