Brequinar sodium

Name: Brequinar sodium
Brand: Tocris Bioscience
SKU: 6196

Tocris Bioscience, part of Bio-Techne | Catalog # 6196

Citations (17)

COA / SDS

Potent and selective DHODH inhibitor

Key Product Details

Description:	Potent and selective DHODH inhibitor
Alternative Names:	BRQ,DuP 785,NSC 368390
Chemical Name:	6-Fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid sodium
Purity:	≥98% (HPLC)
Molecular Weight:	397.35

View Full Technical Details for Brequinar sodium

Technical Data
Citations

Biological Activity for Brequinar sodium

Brequinar sodium is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor (IC₅₀ = ~20 nM). Causes depletion of pyrimidine nucleotides. Exhibits minimal inhibition against a panel of >400 kinases. Triggers differentiation of AML cell lines (ED₅₀ = ~ 1 μM. Note uridine concentration effects ED₅₀ value). Causes differentiation and depletion of leukemia-initiating cells in vivo. Antimetabolite.

Compound Libraries for Brequinar sodium

Brequinar sodium is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for Brequinar sodium

M. Wt	397.35
Formula	C₂₃H₁₄F₂NO₂Na
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	96201-88-6
PubChem ID	23663964
InChi Key	PZOHOALJQOFNTB-UHFFFAOYSA-M
Smiles	CC1=C(C2=CC(F)=CC=C2N=C1C3=CC=C(C4=C(C=CC=C4)F)C=C3)C(O[Na])=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Brequinar sodium

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	39.73	100
	DMSO	39.73	100

Preparing Stock Solutions for Brequinar sodium

The following data is based on the product molecular weight 397.35.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.52 mL	12.58 mL	25.17 mL
5 mM	0.50 mL	2.52 mL	5.03 mL
10 mM	0.25 mL	1.26 mL	2.52 mL
50 mM	0.05 mL	0.25 mL	0.50 mL

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Reconstitution Calculator

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References for Brequinar sodium

References are publications that support the biological activity of the product.

Sykes Inhibition of dihydroorotate dehydrogenase overcomes differentiation blockade in acute myeloid leukemia. Cell 2016 PMID: 27641501
Peters Inhibition of pyrimidine de novo synthesis by DUP-785 (NSC 368390). Invest.New Drugs 1987 PMID: 2822596
Arteaga Phase I clinical and pharmacokinetic trial of Brequinar sodium (DuP 785; NSC 368390). Cancer Res. 1989 PMID: 2743343