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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $55 | In Stock | |
2 mg | $81 | In Stock | |
5 mg | $126 | In Stock | |
10 mg | $207 | In Stock | |
25 mg | $409 | 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 |
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. |
Alias | HS10160, SHR3162 |
Molecular Weight | 472.4 |
Formula | C22H16F4N6O2 |
Cas No. | 1358715-18-0 |
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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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