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Fluzoparib

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Catalog No. T8806Cas No. 1358715-18-0
Alias SHR3162, HS10160

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

Fluzoparib

Fluzoparib

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Purity: 99.63%
Catalog No. T8806Alias SHR3162, HS10160Cas No. 1358715-18-0
Fluzoparib (SHR3162) is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$55In StockIn Stock
2 mg$81In StockIn Stock
5 mg$126In StockIn Stock
10 mg$207In StockIn Stock
25 mg$409In StockIn Stock
50 mg$595-In Stock
100 mg$866-In Stock
500 mg$1,770-In Stock
1 mL x 10 mM (in DMSO)$148In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.63%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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.
SynonymsSHR3162, HS10160
Chemical Properties
Molecular Weight472.4
FormulaC22H16F4N6O2
Cas No.1358715-18-0
SmilesFc1ccc(Cc2n[nH]c(=O)c3ccccc23)cc1C(=O)N1CCn2nc(nc2C1)C(F)(F)F
Relative Density.1.59 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 88.33 mg/mL (186.98 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.99 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1169 mL10.5843 mL21.1685 mL105.8425 mL
5 mM0.4234 mL2.1169 mL4.2337 mL21.1685 mL
10 mM0.2117 mL1.0584 mL2.1169 mL10.5843 mL
20 mM0.1058 mL0.5292 mL1.0584 mL5.2921 mL
50 mM0.0423 mL0.2117 mL0.4234 mL2.1169 mL
100 mM0.0212 mL0.1058 mL0.2117 mL1.0584 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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