Molecular Weight(MW): 268.02
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.
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|Description||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 exerts its anti-proliferative effect, at least partially, through interference with glucose 6 phosphate dehydrogenase (G6PD), a key enzyme in the pentose phosphate pathway, responsible for maintaining adequate levels of the major cellular reductant, NADPH. RRx-001 affects glucose and G6PD enzyme activity in three different cancer cell lines namely Hep G2, CACO-2, and HT-29. RRx-001 induced G6PD inhibition and increased glucose consumption in a concentration dependent fashion. RRx-001 induces p53 and PARP-1 via generation of ROS/RNS. It exerts anticancer activity, at least in part, by interfering with 3 crucial metabolic demands of rapidly proliferating cells: bioenergetics, macromolecular biosynthesis, and manipulation of cellular cytosolic redox homeostasis. RRx-001 mediates nuclear translocation of Nrf2 and the activation of expression of its downstream enzymes HO-1 and NQO1 in tumor cells. Apart from epigenetic alterations, RRx-001 acts via pleiotropic mechanisms including redox signaling and redox-induced dysregulation of many different signal pathways such as Nrf2, p53, PARP cleavage, HIF1 alpha, and G6PD activity. It also triggers p53 and p21 activity in response to double-stranded DNA breaks as well as deregulates cancer cellular energetics and metabolism. RRx-001 is a potent activator of the Nrf2-ARE signaling pathway via ROS/RNS generation.
|In vivo||RRx-001 shows promise for short-term blood flow redistribution in tumors with a pericyte- and α-SMA-rich vasculature. RRx-001 monotherapy is well tolerated, with no dose-limiting toxicities. It not only facilitates nuclear translocation of Nrf2, but also upregulates endogenous Nrf2 expression in SCC VII tumors in mice.|
|In vitro||DMSO||53 mg/mL (197.74 mM)|
|Ethanol||23 mg/mL (85.81 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02215512||Active not recruiting||Brain Metastases||EpicentRx Inc.||February 6 2015||Phase 1|
|NCT02801097||Recruiting||Malignant Solid Tumor|Metastatic Cancer|Advanced Cancer||EpicentRx Inc.||August 30 2016||Phase 1|
|NCT02518958||Active not recruiting||Malignant Solid Tumor|Lymphoma||EpicentRx Inc.||July 21 2015||Phase 1|
|NCT02489903||Recruiting||Small Cell Carcinoma|Carcinoma Non-Small-Cell Lung|Neuroendocrine Tumors|Ovarian Epithelial Cancer||EpicentRx Inc.||June 2015||Phase 2|
|NCT02096354||Active not recruiting||Colorectal Neoplasms||EpicentRx Inc.||May 2014||Phase 2|
|NCT02096341||Terminated||Malignant Solid Tumor|Lymphomas||EpicentRx Inc.||April 2014||Phase 1|
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