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Fluzoparib

Catalog No. T8806 CAS 1358715-18-0

Synonyms: HS10160, SHR3162

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

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Fluzoparib, CAS 1358715-18-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 55.00
2 mg	In stock	$ 81.00
5 mg	In stock	$ 126.00
10 mg	In stock	$ 207.00
25 mg	In stock	$ 409.00
50 mg	In stock	$ 595.00
100 mg	In stock	$ 866.00
500 mg	In stock	$ 1,770.00
1 mL * 10 mM (in DMSO)	In stock	$ 148.00

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Purity: 99.38%

Purity: 98.29%

Biological Description

Chemical Properties

Storage & Solubility Information

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	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

Solubility Information

DMSO: 94 mg/mL (198.98 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Prostate Cancer Compound Library Orally Active Compound Library FDA-Approved & Pharmacopeia Drug Library NO PAINS Compound Library Approved Drug Library Anti-Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Fluzoparib 1358715-18-0 Chromatin/Epigenetic DNA Damage/DNA Repair PARP homologous recombination repair Inhibitor poly ADP ribose polymerase inhibit ovarian SHR-3162 PARP1 HS 10160 HS-10160 HS10160 Fuzuloparib SHR3162 cancer SHR 3162 inhibitor

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