Fluzoparib 是口服活性PARP1抑制剂，IC50为1.46±0.72? nM，在体内具有良好的药代动力学特性，具有抗肿瘤活性，可用于癌症研究。它选择性地抑制同源重组修复 (HR) 缺陷细胞的增殖，并使 HR 缺陷细胞对细胞毒性药物敏感。

fluzoparib is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours.

Fluzoparib potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2 /M arrest, and apoptosis in homologous recombination repair (HR)-deficient cells.?Fluzoparib preferentially inhibited the proliferation of HR-deficient cells and sensitized both HR-deficient and HR-proficient cells to cytotoxic drugs.?Notably, fluzoparib showed good pharmacokinetic properties, favorable toxicity profile, and superior antitumor activity in HR-deficient xenografts models.?Furthermore, fluzoparib in combination with apatinib or with apatinib plus paclitaxel elicited significantly improved antitumor responses without extra toxicity.

In vitro experiments in NSCLC cell lines along with in vivo experiments using an NSCLC xenograft mouse model demonstrated the radiosensitization effect of fluzoparib.?The underlying mechanisms involved increased apoptosis, cell-cycle arrest, enhanced irradiation-induced DNA damage, and delayed DNA-damage repair.

1358715-18-0

C22H16F4N6O2

472.404

HS10160;SHR3162;氟唑帕利

DMSO:94 mg/mL (198.98 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years