| Description | Fluzoparib (SHR3162) is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours. |
| In vitro | 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 vivo | 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. |
| Target activity | PARP1:1.46±0.72 nM (IC50) |
| Synonyms | HS10160, SHR3162, 氟唑帕利 |
| molecular weight | 472.4 |
| Molecular formula | C22H16F4N6O2 |
| CAS | 1358715-18-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 94 mg/mL (198.98 mM) |
| References | 1. Wang L , Yang C , Xie C , et al. Pharmacologic characterization of fluzoparib, a novel poly(ADP‐ribose) polymerase inhibitor undergoing clinical trials[J]. Cancer Science, 2019. 2. Hu X X , Li L , Li D R , et al. Synergism of PARP inhibitor fluzoparib (HS10160) and MET inhibitor HS10241 in breast and ovarian cancer cells[J]. Zhonghua fu chan ke za zhi, 2017, 41(9):579-583. |