2017年11月20日星期一

RRx-001|RRx001|PI3Kalpha inhibitor

RRx-001|RRx001|PI3Kalpha inhibitor

DC Chemicals, Website: www.dcchemicals.com

Product Name: RRx-001|Cas Number: 925206-65-1| Catalog Number: DC10036|Other Nmaes: RRx 001,RRx001

RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia.

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).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. 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.

没有评论:

发表评论