Brequinar sodium
Chemical Name: 6-Fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid sodium
Purity: ≥99%
Biological Activity
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.Technical Data
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.
Background References
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Phase I clinical and pharmacokinetic trial of Brequinar sodium (DuP 785; NSC 368390).
Arteaga
Cancer Res., 1989;49:4648 -
Inhibition of dihydroorotate dehydrogenase overcomes differentiation blockade in acute myeloid leukemia.
Sykes et al.
Cell, 2016;167:171 -
Inhibition of pyrimidine de novo synthesis by DUP-785 (NSC 368390).
Peters et al.
Invest.New Drugs, 1987;5:235
Product Datasheets
Citations for Brequinar sodium
The citations listed below are publications that use Tocris products. Selected citations for Brequinar sodium include:
3 Citations: Showing 1 - 3
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Proof-of-principle studies on a strategy to enhance nucleotide imbalance specifically in cancer cells.
Authors: Juan Et al.
Cell Death Discov 2022;8:464
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DHODH inhibition modulates glucose metabolism and circulating GDF15, and improves metabolic balance.
Authors: Sonia Et al.
iScience 2021;24:102494
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Inhibition of the de novo pyrimidine biosynthesis pathway limits ribosomal RNA transcription causing nucleolar stress in glioblastoma cells.
Authors: Jessica A Et al.
PLoS Genet 2020;16:e1009117
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