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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
Technical Data for Brequinar sodium
|Storage||Store at +4°C|
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 Data for Brequinar sodium
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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||0.5 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|
Product Datasheets for Brequinar sodium
References for Brequinar sodium
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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3 Citations for Brequinar sodium
Citations are publications that use Tocris products. Selected citations for Brequinar sodium include:
Sonia et al (2021) DHODH inhibition modulates glucose metabolism and circulating GDF15, and improves metabolic balance. iScience 24 102494 PMID: 34113829
Juan et al (2022) Proof-of-principle studies on a strategy to enhance nucleotide imbalance specifically in cancer cells. Cell Death Discov 8 464 PMID: 36424385
Jessica A et al (2020) Inhibition of the de novo pyrimidine biosynthesis pathway limits ribosomal RNA transcription causing nucleolar stress in glioblastoma cells. PLoS Genet 16 e1009117 PMID: 33201894
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