同义名 :	DuP785 sodium; NSC 368390 sodium; NSC 368390; DUP-785; BRQ; Bipenquinate
	CAS号 :	96201-88-6
	货号 :	A207630
	分子式 :	C23H14F2NNaO2
	纯度 :	95%
	分子量 :	397.35
	MDL号 :	MFCD22648381
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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[1]. Brequinar sodium 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[2]. Moreover, combination of brequinar sodium 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[3].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.52mL 0.50mL 0.25mL	12.58mL 2.52mL 1.26mL	25.17mL 5.03mL 2.52mL

参考文献

[1]Boschi D, Pippione AC, Sainas S, Lolli ML. Dihydroorotate dehydrogenase inhibitors in anti-infective drug research. Eur J Med Chem. 2019;183:111681 [2]Peters GJ. Re-evaluation of Brequinar sodium, a dihydroorotate dehydrogenase inhibitor. Nucleosides Nucleotides Nucleic Acids. 2018;37(12):666-678 [3]Dorasamy MS, Ab A, Nellore K, Wong PF. Synergistic inhibition of melanoma xenografts by Brequinar sodium and Doxorubicin. Biomed Pharmacother. 2019;110:29-36