RRX-001
- Product Name
- RRX-001
- CAS No.
- 925206-65-1
- Chemical Name
- RRX-001
- Synonyms
- ABDNAZ;RRX-001;[14C]-Rrx-001;RRX 001;RRX001;RRx-001 ，S8405;RRx-001 (ABDNAZ);RRX-001, 10 mM in DMSO;2-Bromo-1-(3,3-dinitro-1-azetidinyl)ethanone;2-Bromo-1-(3,3-dinitroazetidin-1-yl)ethanone;2-bromo-1-(3,3-dinitroazetidin-1-yl)ethan-1-one
- CBNumber
- CB92658200
- Molecular Formula
- C5H6BrN3O5
- Formula Weight
- 268.02
- MOL File
- 925206-65-1.mol
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
- InChI
- InChI=1S/C5H6BrN3O5/c6-1-4(10)7-2-5(3-7,8(11)12)9(13)14/h1-3H2
- InChIKey
- JODKFOVZURLVTG-UHFFFAOYSA-N
- SMILES
- C(=O)(N1CC([N+]([O-])=O)([N+]([O-])=O)C1)CBr
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..…
N-Bromosuccinimide Price
- Product number
- 28846
- Product name
- RRx-001
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 28846
- Product name
- RRx-001
- Packaging
- 25mg
- Price
- $586
- Updated
- 2024/03/01
- Product number
- 28846
- Product name
- RRx-001
- Packaging
- 5mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 28846
- Product name
- RRx-001
- Packaging
- 10mg
- Price
- $321
- Updated
- 2024/03/01
- Product number
- CS-5286
- Product name
- RRx-001
- Purity
- 99.71%
- Packaging
- 5mg
- Price
- $144
- Updated
- 2021/12/16
RRX-001 Chemical Properties,Usage,Production
Uses
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity[1]. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α[2]. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity[3].
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 |
IC 50
Plasmodium
References
[1] Das DS, et al. A novel hypoxia-selective epigenetic agent RRx-001 triggers apoptosis and overcomes drug resistance in multiple myeloma cells. Leukemia. 2016 Nov;30(11):2187-2197. DOI:10.1038/leu.2016.96
[2] 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. DOI:10.1186/s12936-015-0720-5
[3] Cabrales P, et al. RRx-001 Acts as a Dual Small Molecule Checkpoint Inhibitor by Downregulating CD47 on Cancer Cells and SIRP-α on Monocytes/Macrophages. Transl Oncol. 2019 Apr;12(4):626-632. DOI:10.1016/j.tranon.2018.12.001
RRX-001 Preparation Products And Raw materials
Raw materials
Preparation Products
RRX-001 Suppliers
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View Lastest Price from RRX-001 manufacturers
- Product
- RRX-001 925206-65-1
- Price
- US $7.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2020-02-18