中文名称: | 布喹那 | ||||
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英文名称: | Brequinar | ||||
别名: | 布喹那;6-氟-2-(2’-氟联苯-4-基)-3-甲基喹啉-4-羧酸 DUP785; 6-fluoro-2-(2'-fluoro-[1,1'-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid | ||||
CAS No: | 96187-53-0 | 分子式: | C23H15F2NO2 | 分子量: | 375.37 |
CAS No: | 96187-53-0 | ||||
分子式: | C23H15F2NO2 | ||||
分子量: | 375.37 | ||||
EINEC: | 368390 | ||||
EINEC: | 368390 |
基本信息
产品编号:B10417 |
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产品名称:Brequinar |
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CAS: |
96187-53-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
375.37 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
37mg/mL (98.56mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.6640mL |
13.3202mL |
26.6404mL |
5mM |
0.5328mL |
2.6640mL |
5.3281mL |
10mM |
0.2664mL |
1.3320mL |
2.6640mL |
50mM |
0.0533mL |
0.2664mL |
0.5328mL |
生物活性
产品描述 |
一种有效的DHODH抑制剂。 |
靶点/IC50 |
DHODH |
20 nM |
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体外研究 |
Brequinar reduces virus progeny production by >90%, with EC50 of 17nM. Brequinar (5μM) 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 EC50 of 78nM in the CFI assay. Brequinar (5μM) 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 (5μM) suppresses the luciferase activities from both the WT and NS5 mutant replicons. Brequinar sodium effectively prevents the increase in PyNTP levels with an IC50 of 0.26μM. Brequinar sodium effectively inhibits cell proliferation with an IC50 of 0.26μM. Brequinar sodium inhibits autophosphorylation of p56lck with IC50 of 70μM; inhibition is 39, 41, and 60% for 25, 50, and 100μM Brequinar sodium,respectively. Brequinar sodium also inhibits the phosphorylation by p56lck of the exogenous substrate, histone 2B, with an IC50 of 70μM; inhibition is 10, 43, 59, and 86% for 25,50, 100, and 200μM Brequinar sodium,respectively. Brequinar sodium inhibits autophosphorylation of p59fyn with an IC50 of 105μM; inhibition is 0, 17, 48, and 65% for 25,50,100, and 200μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p59fyn of histone 2B with an IC50 of 20μM; inhibition is 26, 54, 79, 83, and 84% for 10, 25, 50, 100, and 200μM Brequinar sodium, respectively. |
体内研究 |
Brequinar sodium-treated (10-20mg/kg/day) mice has a 31% reduction in percentage of packed cell volume compared with urequinar sodium-treated (10-20mg/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 (10-20mg/kg/day) in combination with uridine (1000-2000mg/kg/day) prevents anemia, and the hematocrits remain at levels (61-63%) comparable with those of untreated controls. |
推荐实验方法(仅供参考)
激酶实验: |
Immunoprecipitated p59fyn or p56lck from CTLL-4 cells or LSTRA cells (5×106) is preincubated with various concentrations of BQR in the PTK buffer (50 mM HEPES (pH 7.4), 10mM MgCl2, and 10mM MnCl2) on ice for 10min. Exogenous substrate,histone 2B (2μg), is added and, after 10min, the reaction is initiated by addition of 10μCi [γ-32P]ATP. After incubation at 20℃ for 10min, the reaction mixture is subjected to electrophoresis in a 12.5% SDS-polyacrylamide gel.Phosphorylation of the kinase and the exogenous substrate is analyzed by autoradiography. |
细胞实验: |
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The neutral-red uptake assay is used to evaluate cell viability. BSC-40 cells are seeded in 96-well plates in the presence of concentrations of Brequinar ranging from 0.01μM to 75μM for 24h.Control cells are incubated with 0.1% DMSO. Neutral red is methanol/acetic acid-extracted from cells and is quantitated at an absorbance of 490nm (A490). All measurements expressed the average of four independent assays. |
动物实验: |
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Brequinar is administered once daily by i.p. injection, while uridine is administered twice daily.Mice are bled through the orbital vein using a microhematocrit capillary tube, and the blood is centrifuged for 10min at 550 × g. The percentage of packed cell volumes is determined with a microhematocrit capillary tube reader. All mice are killed 4 h after receiving their last dose of Brequinar or uridine. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )