Chemical Name: 6-Fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid sodium
Biological ActivityBrequinar 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.
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.
Phase I clinical and pharmacokinetic trial of Brequinar sodium (DuP 785; NSC 368390).
Cancer Res., 1989;49:4648
Inhibition of dihydroorotate dehydrogenase overcomes differentiation blockade in acute myeloid leukemia.
Sykes et al.
Inhibition of pyrimidine de novo synthesis by DUP-785 (NSC 368390).
Peters et al.
Invest.New Drugs, 1987;5:235
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