| Description: |
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). |
| Target: |
IC50 value: 0.14 ± 0.04 ug/ml [1]
Target: G6PD |
| 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] |
| In 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] |
| References: |
[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. |
