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Fluzoparib (SHR3162) is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $55 | In Stock | In Stock | |
| 2 mg | $81 | In Stock | In Stock | |
| 5 mg | $126 | In Stock | In Stock | |
| 10 mg | $207 | In Stock | In Stock | |
| 25 mg | $409 | In Stock | In Stock | |
| 50 mg | $595 | - | In Stock | |
| 100 mg | $866 | - | In Stock | |
| 500 mg | $1,770 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $148 | In Stock | In Stock |
| Description | Fluzoparib (SHR3162) is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours. |
| Targets&IC50 | PARP1:1.46±0.72 nM (IC50) |
| 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. |
| Synonyms | SHR3162, HS10160 |
| Molecular Weight | 472.4 |
| Formula | C22H16F4N6O2 |
| Cas No. | 1358715-18-0 |
| Smiles | Fc1ccc(Cc2n[nH]c(=O)c3ccccc23)cc1C(=O)N1CCn2nc(nc2C1)C(F)(F)F |
| Relative Density. | 1.59 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| 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: 94 mg/mL (198.98 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.99 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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