Fluzoparib (SHR-3162) | PARP inhibitor | CAS 1358715-18-0

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Quality Control

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

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COA
NMR
SDS
Datasheet

99.88

Related Targets	HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF
Other PARP Products	XAV-939 AZD5305 (Saruparib) Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (198.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.58mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.58mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	472.40	Formula	C₂₂H₁₆F₄N₆O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1358715-18-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	HS10160			Smiles	FC1=CC=C(CC2=NNC(=O)C3=C2C=CC=C3)C=C1C(=O)N4CC[N]5N=C(N=C5C4)C(F)(F)F

Mechanism of Action

Targets/IC₅₀/Ki	PARP
In vitro	Upon exposure to fluzoparib (SHR-3162), all four NSCLC cell lines (A549, H460, H1299, and PC9) show decreased viability in a time- and dose-dependent manner. It acts synergistically to inhibit cell growth and promote apoptosis among lung cancer cells.
In vivo	An H460 cell xenograft mouse model is established to study the in vivo effects of fluzoparib (SHR-3162) and RT on tumor growth and survival. Treatment with RT + this compound more effectively delayed tumor growth than treatment with either RT or it individually. When combined with RT, it conferres a significant survival benefit with no evidence of toxicity.
References	[1] https://pubmed.ncbi.nlm.nih.gov/30949414/ [2] https://pubmed.ncbi.nlm.nih.gov/31786739/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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	Completed	Renal Impairment	Jiangsu HengRui Medicine Co. Ltd.	November 9 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

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Fluzoparib (SHR-3162) PARP inhibitor

Chemical Structure

Molecular Weight: 472.40