布喹那
Brequinar
CAS: 96187-53-0
Molecular Formula: C23H15F2NO2
布喹那 - Names and Identifiers
| Name | Brequinar |
| Synonyms | BPQ Brequinar Biphenquinate 6-fluoro-2-(2'-fluorobiphenyl-4-yl)-3-Methylquinoline-4-carboxyl 6-fluoro-2-(2'-fluorobiphenyl-4-yl)-3-methylquinoline-4-carboxylic acid 6-Fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid 6-Fluoro-2-(2'-fluoro-[1,1'-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid 4-Quinolinecarboxylic acid, 6-fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-Methyl- |
| CAS | 96187-53-0 |
布喹那 - Physico-chemical Properties
| Molecular Formula | C23H15F2NO2 |
| Molar Mass | 375.37 |
| Melting Point | 355-357℃ (N,N-dimethylformamide water ) |
| Appearance | powder to crystal |
| Color | White to Light yellow |
| pKa | pKa 4.45(H2O t=RT I=0.10) (Uncertain) |
| Storage Condition | 2-8°C |
| In vitro study | Brequinar reduces virus progeny production by >90%, with EC 50 of 17 nM. Brequinar (5 μM) also inhibits other orthopoxviruses, and blocks virus DNA replication. Brequinar does not affect virus early gene expression, but has a severe effect on the late stage of the virus cycle. Brequinar reduces the level of envelope protein production and the viral titer in a dose-dependent manner, with EC 50 of 78 nM in the CFI assay. Brequinar (5 μM) inhibits viral RNA synthesis. Brequinar has antiviral effect, but the effect is reversed by pyrimidine. Brequinar-resistant viruses can be selected in cell culture. Brequinar (5 μM) suppresses the luciferase activities from both the WT and NS5 mutant replicons. Brequinar sodium effectively prevents the increase in PyNTP levels with an IC 50 of 0.26 μM. Brequinar sodium effectively inhibits cell proliferation with an IC 50 of 0.26 μM. Brequinar sodium inhibits autophosphorylation of p56 lck with IC 50 of 70 μM; inhibition is 39, 41, and 60% for 25, 50, and 100 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p56 lck of the exogenous substrate, histone 2B, with an IC 50 of 70 μM; inhibition is 10, 43, 59, and 86% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium inhibits autophosphorylation of p59 fyn with an IC 50 of 105 μM; inhibition is 0, 17, 48, and 65% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p59 fyn of histone 2B with an IC 50 of 20 μM; inhibition is 26, 54, 79, 83, and 84% for 10, 25, 50, 100, and 200 μM Brequinar sodium, respectively. |
| In vivo study | Brequinar sodium-treated (10-20 mg/kg/day) mice has a 31% reduction in percentage of packed cell volume compared with untreated BALB/c mice. Brequinar sodium reduces UTP and CTP levels in bone marrow cells by 30 and 25%, respectively. Brequinar sodium (10-20 mg/kg/day) in combination with uridine (1000-2000 mg/kg/day) prevents anemia, and the hematocrits remain at levels (61-63%) comparable with those of untreated controls. |
布喹那 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.664 ml | 13.32 ml | 26.64 ml |
| 5 mM | 0.533 ml | 2.664 ml | 5.328 ml |
| 10 mM | 0.266 ml | 1.332 ml | 2.664 ml |
| 5 mM | 0.053 ml | 0.266 ml | 0.533 ml |
Last Update：2024-01-02 23:10:35
布喹那 - Reference Information
| biological activity | Brequinar (NSC DuP-785,) is a dihydroorotate dehydrogenase DHODH inhibitor with an IC50 of about 20 nM in vitro. |
| Target | Value |
| DHODH () | 20 nM |
Last Update：2024-04-09 21:54:55
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Product Name: 6-Fluoro-2-(2'-fluoro-[1,1'-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid Visit Supplier Webpage Request for quotationCAS: 96187-53-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Brequinar Visit Supplier Webpage Request for quotationCAS: 96187-53-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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