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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
If you know of a relevant reference for Brequinar sodium, please let us know.
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