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Brequinar sodium

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Catalog No. T8332Cas No. 96201-88-6
Alias NSC 368390 sodium, DuP785 sodium

Bipenquinate is a potent and selective inhibitor of dihydroorotate dehydrogenase (DHODH) with IC50 of 20 nM, blocking de novo pyrimidine biosynthesis.

Brequinar sodium

Brequinar sodium

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Purity: 98.16%
Catalog No. T8332Alias NSC 368390 sodium, DuP785 sodiumCas No. 96201-88-6
Bipenquinate is a potent and selective inhibitor of dihydroorotate dehydrogenase (DHODH) with IC50 of 20 nM, blocking de novo pyrimidine biosynthesis.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$33In StockIn Stock
5 mg$60In StockIn Stock
10 mg$98In StockIn Stock
25 mg$181In StockIn Stock
50 mg$236In StockIn Stock
100 mg$331In StockIn Stock
200 mg$467In StockIn Stock
1 mL x 10 mM (in DMSO)$71In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.16%
Appearance:Solid
Color:White
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Product Introduction

Brequinar sodium AI Summary
Brequinar sodium is a potent inhibitor of human recombinant dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value as low as 8.0 nM and a Ki value of 12.0 nM. It demonstrates significant antiproliferative activity in human lymphocytes, as evidenced by an IC50 value of 15.0 nM in the mixed lymphocyte reaction test. Additionally, Brequinar sodium shows broad-spectrum growth inhibition across various human tumor cell lines, with GI50 values ranging from 56.62 nM to 155238.7 nM, highlighting its potential as an anti-cancer agent. It also exhibits cytotoxic effects on A375, Hep3B, HCT116, BxPC3, WI38, HT-29, and MDA-MB-231 cell lines, with varying IC50 values, and inhibits DHODH activity significantly, achieving up to 97.29% inhibition at 10 µM. Furthermore, Brequinar sodium demonstrates notable antiviral properties, particularly against SARS-CoV-2, by reducing virus-induced cytotoxicity in Caco-2 and VERO-6 cells. Its SARS-CoV-2 3CL-Pro protease inhibition, however, is minimal at 0.795% at 20 µM. The compound also increases IFN-alpha mediated responses in HEK-293 cells with an EC50 of 54.95 nM. These multifaceted biological activities suggest that Brequinar sodium is a promising candidate for further investigations in cancer and antiviral therapies..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Bipenquinate is a potent and selective inhibitor of dihydroorotate dehydrogenase (DHODH) with IC50 of 20 nM, blocking de novo pyrimidine biosynthesis.
SynonymsNSC 368390 sodium, DuP785 sodium
Chemical Properties
Molecular Weight397.36
FormulaC23H14F2NNaO2
Cas No.96201-88-6
Smiles[Na+].Cc1c(nc2ccc(F)cc2c1C([O-])=O)-c1ccc(cc1)-c1ccccc1F
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 3.98 mg/mL (10.02 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5166 mL12.5830 mL25.1661 mL125.8305 mL
5 mM0.5033 mL2.5166 mL5.0332 mL25.1661 mL
10 mM0.2517 mL1.2583 mL2.5166 mL12.5830 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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