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| Bipenquinate Basic information |
Product Name: | Bipenquinate | Synonyms: | Bipenquinate;Brequinar sodium;2-(2'-Fluoro-1,1'-biphenyl-4-yl)-3-methyl-6-fluoroquinoline-4-carboxylic acid sodium salt;Dup-785;NSC-368390;SODIUM 6-FLUORO-2-(2-FLUORO-[1,1-BIPHENYL]-4-YL)-3-METHYLQUINOLINE-4-CARBOXYLATE;6-Fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid sodium;6-fluoro-2-[4-(2-fluorophenyl)phenyl]-3-methylquinoline-4-carboxylate | CAS: | 96201-88-6 | MF: | C23H14F2NNaO2 | MW: | 0 | EINECS: | 604-604-1 | Product Categories: | | Mol File: | 96201-88-6.mol | |
| Bipenquinate Chemical Properties |
Melting point | >360° | storage temp. | under inert gas (nitrogen or Argon) at 2-8°C | solubility | Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to 15 mg/ml with warming) | form | solid | color | Off-white or white | 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. |
| Bipenquinate Usage And Synthesis |
Description | 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 | Uses | Antineoplastic. | Definition | ChEBI: Brequinar sodium is an organic sodium salt of brequinar. It has a role as an anticoronaviral agent, an antineoplastic agent, an antiviral agent, an EC 1.3.5.2 [dihydroorotate dehydrogenase (quinone)] inhibitor, an immunosuppressive agent, a pyrimidine synthesis inhibitor and an antimetabolite. It contains a brequinar(1-). | storage | Store at +4°C | References | 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 |
| Bipenquinate Preparation Products And Raw materials |
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