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Brequinar sodium | Dihydroorotate dehydrogenase inhibitor, antiviral

CAS:
96201-88-6
Catalog Number:
10-3965
Activity:
Dihydroorotate dehydrogenase inhibitor, antiviral
Chemical Name:
6-Fluoro-2-[4-(2-fluorophenyl)phenyl]-3-methylquinoline-4-carboxylic acid sodium salt
Alternate Name:
DuP-785; NSC 368390
Molecular Weight:
397.35
Molecular Formula:
C23H14F2NO2•Na
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to 15 mg/ml with warming)
Physical Properties:
Off-white or white solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20° C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
Shipping Code:
RT

Brequinar sodium (96201-88-6) is an inhibitor of dihydroorotate dehydrogenase (DHODH)1,2 with IC50’s between 0.2 and 5.8 µM in various cell lines3 and 20 nM in isolated enzyme4. It reduced leukemic cell burden, decreased levels of leukemia-initiating cells, and improved survival in human and mouse models of acute myeloid leukemia.4 Brequinar displayed broad antiviral activity against flaviviruses, positive-strand RNA alphaviruses, negative-strand RNA rhabdoviruses, Influenza A and B viruses, and HIV.5-7

References/Citations:

1) Chen et al. (1986) Mechanism of action of the novel anticancer agent 6-fluoro-2-(2’-fluoro-1,1’-biohenyl-4-yl)-3-methyl-4-quinolinecarboxylic acid sodium salt (NSC 368390): inhibition of de novo pyrimidine nucleotide biosynthesis; Cancer Res., 46 5014
2) Peters et al. (1990) In vivo inhibition of the pyrimidine de novo enzyme dihydroorotic aicd dehydrogenase by brequinar sodium (DUP-785; NSC 368390) in mice and patients; Cancer Res., 50 4644
3) De Kant et al. (1989) The relation between inhibition of cell growth and of dihydroorotic acid dehydrogenase by brequinar sodium; Cancer Lett., 46 123
4) Sykes et al. (2016) Inhibition of Dihydroorotate Overcomes Differentiation Blockade in Acute Myeloid Leukemia; Cell, 167 171
5) Qing et al. (2010) Characterization of Dengue Virus Resistance to Brequinar in Cell Culture; Antimicrob. Agents Chemother., 54 3686
6) Andersen et al. (2019) Novel Antiviral Activities of Obatoclax, Emetine, Niclosamide, Brequinar, and Homoharringtonine; Viruses, 11 E964
7) Park et al. (2020) Identification and Characterization of Novel Compounds with Broad-Spectrum Antiviral Activity against Influenza A and B Viruses; J. Virol., 94 e02149

Brequinar sodium | Dihydroorotate dehydrogenase inhibitor, antiviral is also available in the Cellular Metabolism Library.
CAS:
96201-88-6
Catalog Number:
10-3965
Activity:
Dihydroorotate dehydrogenase inhibitor, antiviral
Chemical Name:
6-Fluoro-2-[4-(2-fluorophenyl)phenyl]-3-methylquinoline-4-carboxylic acid sodium salt
Alternate Name:
DuP-785; NSC 368390
Molecular Weight:
397.35
Molecular Formula:
C23H14F2NO2•Na
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to 15 mg/ml with warming)
Physical Properties:
Off-white or white solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20° C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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