RRX-001 Property

Boiling point:

473.0±45.0 °C(Predicted)

Density 

1.98±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 2 mg/ml

form 

A solid

pka

-2.07±0.20(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H311Toxic in contact with skin

H331Toxic if inhaled

H341Suspected of causing genetic defects

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P308+P313IF exposed or concerned: Get medical advice/attention.

P310Immediately call a POISON CENTER or doctor/physician.

P330Rinse mouth.

P361Remove/Take off immediately all contaminated clothing.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

RRX-001 Chemical Properties,Usage,Production

Biological Activity

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

in vitro

RRx-001 exerts its antiproliferative effect by interfering with glucose 6 phosphate dehydrogenase (G6PD), a key enzyme in the pentose phosphate pathway. RRx-001 induces p53 and PARP-1 through ROS/RNS generation. It exerts its anticancer activity by interfering and disrupting 3 crucial metabolic demands in rapidly proliferating cells: bioenergetics, macromolecular biosynthesis and manipulation of cellular cytoplasmic redox homeostasis.RRx-001 also mediates the nuclear translocation of Nrf2 and the expression of its downstream HO-1 and NQO1 in tumor cells.

in vivo

RRx-001 has a short-term blood flow redistribution effect in tumors enriched in pericytes and α-SMA vessels.It was well tolerated without dose-limiting toxic side effects. In mice, it not only promoted nuclear transport of Nrf2, but also upregulated the expression of endogenous Nrf2 in SCC VII tumors.

target

Target	Value
G6PD ()
Nrf2-ARE