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
- Molecular Weight:
- 268.02
- MDL Number:
- MFCD25976849
- MOL File:
- 925206-65-1.mol
| Product description | Number | Pack Size | Price |
| RRx-001 | 28846 | 1mg | $44 |
| RRx-001 | 28846 | 25mg | $586 |
| RRx-001 | 28846 | 5mg | $172 |
| RRx-001 | 28846 | 10mg | $321 |
| RRX-001 95.00% | API0045691 | 5MG | $496.6 |
| More product size | |||
| 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 |
| FDA UNII | 7RPW6SU9SC |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS06,GHS08 |
|---|---|
| Signal word | Danger |
| Hazard statements | H301-H311-H331-H341 |
| Precautionary statements | P201-P202-P261-P264-P270-P271-P280-P302+P352-P304+P340-P308+P313-P310-P330-P361-P403+P233-P405-P501 |
RRX-001 price More Price(16)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 28846 | RRx-001 | 925206-65-1 | 1mg | $44 | 2024-03-01 | Buy |
| Cayman Chemical | 28846 | RRx-001 | 925206-65-1 | 25mg | $586 | 2024-03-01 | Buy |
| Cayman Chemical | 28846 | RRx-001 | 925206-65-1 | 5mg | $172 | 2024-03-01 | Buy |
| Cayman Chemical | 28846 | RRx-001 | 925206-65-1 | 10mg | $321 | 2024-03-01 | Buy |
| American Custom Chemicals Corporation | API0045691 | RRX-001 95.00% | 925206-65-1 | 5MG | $496.6 | 2021-12-16 | Buy |
RRX-001 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29799 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32435 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39035 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +86-18621343501; +undefined18621343501 | product@acmec-e.com | China | 33338 | 58 |
| Young Lively PharminBlock Co.,Ltd | +undefined18600731423 | jason_gao@yl-pharminblock.com | China | 1944 | 58 |
