Home DNA Damage/DNA Repair PARP inhibitor Fluzoparib (SHR-3162) For research use only.

Fluzoparib (SHR-3162)

Synonyms: HS10160

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity, with an IC50 of 1.46±0.72 nM for PARP1.

Fluzoparib (SHR-3162) Chemical Structure

Fluzoparib (SHR-3162) Chemical Structure

CAS: 1358715-18-0

Selleck's Fluzoparib (SHR-3162) has been cited by 1 publication

Purity & Quality Control

Batch: S971201 DMSO] 94 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.88%
99.88

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Signaling Pathway

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Biological Activity

Description

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity, with an IC50 of 1.46±0.72 nM for PARP1.
Targets
PARP [1]
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models 5-6 week-old female Nu/Nu mice
Dosages 1 mg/kg
Administration IG
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05732129 Not yet recruiting
Homologous Recombination Deficiency Alterations Metastatic Colorectal Cancer
Fudan University
 March 1 2023 Phase 2
NCT05032235 Unknown status
Renal Impairment
Jiangsu HengRui Medicine Co. Ltd.
 September 15 2021 Phase 1
NCT04694365 Unknown status
Hepatic Impairment|Healthy Subjects
Jiangsu HengRui Medicine Co. Ltd.
 November 6 2020 Phase 1
NCT04517357 Unknown status
Relapsed Ovarian Cancer
Jiangsu HengRui Medicine Co. Ltd.
 October 16 2020 Phase 2
NCT04659785 Unknown status
Small Cell Lung Cancer Extensive Stage
Tianjin Medical University Second Hospital
 July 1 2020 Phase 1|Phase 2
NCT04400188 Active not recruiting
Small Cell Lung Cancer
Jiangsu HengRui Medicine Co. Ltd.
 June 11 2020 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 472.40 Formula

C22H16F4N6O2
CAS No. 1358715-18-0 SDF --
Smiles FC1=CC=C(CC2=NNC(=O)C3=C2C=CC=C3)C=C1C(=O)N4CC[N]5N=C(N=C5C4)C(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 94 mg/mL ( (198.98 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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