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RRx-001
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RRx-001图片
CAS NO:925206-65-1
规格:98%
分子量:268.02
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
RRX-001是一种有效的葡萄糖-6-磷酸脱氢酶(G6PD)抑制剂。RRX-001具有强抗疟效果,药物敏感性测试表明,抑制寄生虫活性IC50=0.14±0.04ug/ml。
CAS:925206-65-1
分子式:C5H6BrN3O5
分子量:268.02
纯度:98%
存储:Store at -20°C

Background:

RRx-001 is a potent inhibitor of G6PD. RRx-001 shows potent antimalarial, although as a single agent, the drug sensitivity testing indicated that higher dose of RRx-001 was required to inhibited 50 % of the parasite’s activity (IC50 = 0.14 ± 0.04 ug/ml).IC50 value: 0.14 ± 0.04 ug/ml [1]Target: G6PDin vitro: RRx-001 is a novel, systemically non-toxic, epigenetic anticancer agent for multiple tumour types, with activity mediated through increased nitric oxide (NO) production and PPP inhibition. [1]in vivo: RRx-001is a novel, nonexplosive molecule modified from a class of solid rocket propellants, has shown promise as a novel cancer therapeutic agent in a number of cell lines and tumor models. In mouse models, RRx-001 administered intravenously as a single agent was equipotent to cisplatin while better tolerated. RRx-001 also showed activity as a radiosensitizer in both in vitro and in vivo models. The activity of RRx-001 is thought to be associated with a nucleophilic substitution by circulating thiol compounds and covalent binding of RRx-001 to cysteinyl residues in Hb, followed by the generation of nitrogen oxides. [2]




[1]. Yalcin O, et al. From METS to malaria: RRx-001, a multi-faceted anticancer agent with activity in cerebral malaria. Malar J. 2015 May 28;14:218. [2]. Scicinski J, et al. Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent. Drug Metab Dispos. 2012 Sep;40(9):1810-1816.