Fluzoparib (SHR-3162)

For research use only.

Catalog No.S9712 Synonyms: HS10160

Fluzoparib (SHR-3162) Chemical Structure

CAS No. 1358715-18-0

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.

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Biological Activity

Description

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.

Targets
PARP [1]
()
In vitro

All four NSCLC cell lines (A549, H460, H1299, and PC9) shows decreased viability upon exposure to fluzoparib, and the effect is time and dose dependent. Fluzoparib acts synergistically to inhibit cell growth and promote apoptosis among lung cancer cells.[2]

In vivo

An H460 cell xenograft mouse model is established to study the in vivo effects of fluzoparib and RT on tumor growth and survival. Treatment with RT + fluzoparib more effectively delayed tumor growth than treatment with either RT or fluzoparib individually. When combined with RT, fluzoparib conferres a significant survival benefit with no evidence of toxicity.[2]

Protocol

Cell Research:

[2]

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  • Cell lines: human NSCLC cell lines A549, H460, H1299 and PC9
  • Concentrations: 0–800 μM
  • Incubation Time: 24 h, 48 h, 72 h, 96 h
  • Method:

    Cells of all four NSCLC cell lines (A549, H460, H1299 and PC9) are plated in 96-well plates separately, with approximately 2 × 103 cells added to each well. The cells are exposed to fluzoparib at different concentration (0–800 μM) in completed medium for 24, 48, 72, or 96 h. After exposure of the cells to fluzoparib for the indicated time period, the CellTiter 96 Aqueous Non-radioactive Cell Proliferation assay is used to detect cell viability, and IC50 values are calculated. The experiment is performed three times and mean and standard deviation (SD) values are calculated for further statistical analysis of the results.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: 5-6 week-old female Nu/Nu mice
  • Dosages: 1 mg/kg
  • Administration: IG
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (198.98 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 472.40
Formula

C22H16F4N6O2

CAS No. 1358715-18-0
Storage powder
in solvent
Synonyms HS10160

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05032235 Not yet recruiting Drug: Fluzoparib Renal Impairment Jiangsu HengRui Medicine Co. Ltd. September 15 2021 Phase 1
NCT04694365 Recruiting Drug: Fluzoparib Hepatic Impairment|Healthy Subjects Jiangsu HengRui Medicine Co. Ltd. November 6 2020 Phase 1
NCT04517357 Recruiting Drug: Fluzoparib+Apatinib|Drug: Fluzoparib Relapsed Ovarian Cancer Jiangsu HengRui Medicine Co. Ltd. October 16 2020 Phase 2
NCT04659785 Recruiting Drug: Fluzoparib|Drug: Apatinib Small Cell Lung Cancer Extensive Stage Tianjin Medical University Second Hospital July 1 2020 Phase 1|Phase 2
NCT04400188 Recruiting Drug: Fluzoparib|Drug: temozolomide|Biological: SHR-1316 Small Cell Lung Cancer Jiangsu HengRui Medicine Co. Ltd. June 11 2020 Phase 1|Phase 2
NCT04108676 Unknown status Drug: Fluzoparib|Drug: Omeprazole Advanced Solid Tumor Jiangsu HengRui Medicine Co. Ltd.|The Third Xiangya Hospital of Central South University September 7 2019 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID