Brequinar sodium

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Cat.No. 6196 - Brequinar sodium | C23H14F2NO2Na | CAS No. 96201-88-6
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: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

M. Wt 397.35
Formula C23H14F2NO2Na
Storage Store at +4°C
Purity ≥99% (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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 397.35. Batch specific molecular weights may vary from batch to batch due to solvent 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 0.5 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 0.5 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Arteaga (1989) Phase I clinical and pharmacokinetic trial of Brequinar sodium (DuP 785; NSC 368390). Cancer Res. 49 4648 PMID: 2743343

Sykes et al (2016) Inhibition of dihydroorotate dehydrogenase overcomes differentiation blockade in acute myeloid leukemia. Cell 167 171 PMID: 27641501

Peters et al (1987) Inhibition of pyrimidine de novo synthesis by DUP-785 (NSC 368390). Invest.New Drugs 5 235 PMID: 2822596


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Citations for Brequinar sodium

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Literature in this Area

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