| Name | Fluzoparib |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 94 mg/mL (198.98 mM)
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| Keywords | homologous recombination repair | Inhibitor | poly ADP ribose polymerase | inhibit | ovarian | SHR-3162 | Fluzoparib | PARP | PARP1 | HS 10160 | HS-10160 | Fuzuloparib | cancer | SHR 3162 |
| Inhibitors Related | 4'-Methoxychalcone | VPC-70063 | 3-Aminobenzamide | XAV-939 | Niraparib | 3-Methoxybenzamide | NU1025 | Olaparib | Benzamide | OUL35 |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Approved Drug Library | Drug Repurposing Compound Library | Anti-Prostate Cancer Compound Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
