| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 88.33 mg/mL (186.98 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.99 mM), Sonication is recommended.
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| Keywords | SHR-3162 | SHR 3162 | poly ADP ribose polymerase | PARP1 | PARP | ovarian | Inhibitor | inhibit | HS-10160 | HS 10160 | homologous recombination repair | Fuzuloparib | Fluzoparib | cancer |
| Inhibitors Related | BGP-15 | Niraparib tosylate monohyrate | 7-Methylguanine | 3-Aminobenzamide | XAV-939 | Niraparib | AZ9482 | RMC-7977 | RBN-2397 | Olaparib | Benzamide | OUL35 |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |