CAS:96187-53-06-Fluoro-2-(2'-fluoro-[1,1'-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid

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Brequinar 布喹那 Cat No. FB16584Cas No. 96187-53-0

Synonyms: DUP785; NSC 368390

Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses.

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18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6641 mL
- 13.3203 mL
- 26.6406 mL
- 5 mM
- 0.5328 mL
- 2.6641 mL
- 5.3281 mL
- 10 mM
- 0.2664 mL
- 1.3320 mL
- 2.6641 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号	96187-53-0	储存条件	粉末 -20°C 3 年液体 -80°C 12 月
分子式	C23H15F2NO2	运输	蓝冰
分子量	375.37	别名	DUP785; NSC 368390

靶点数据

生物活性

描述Dihydroorotate dehydrogenase (DHODH) is the only redox enzyme of the six enzymes involved in the de novo biosynthesis pathway. It catalyses the oxidation of dihydroorotate (DHO) to orotate (ORO) and the electrons are transferred via the involvement of two cofactors (flavin mononucleotide (FMN) and either nicotinamide adenine dinucleotide (NAD) or ubiquinone (CoQ)) in the respiratory mitochondrial chain^[5]. Brequinar is a potent inhibitor of the mitochondrial DHODH, a rate-limiting enzyme in the pyrimidine de novo nucleotide synthesis. In phase I clinical studies at the maximum tolerated dose (MTD) Brequinar induced a long-term inhibition of DHODH in white blood cells (WBC) and a long-term depletion of plasma uridine^[6]. Moreover, combination of Brequinar with doxorubicin resulted in synergistic and additive cell growth inhibition in melanoma cells. In addition, in vivo studies with this combination of drugs demonstrated an almost 90% tumor regression in nude mice bearing melanoma tumors^[7].