RRx-001
Based on 20 publication(s) in Google Scholar
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. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.79%
- No. CAS: 925206-65-1
- Fòrmula: C5H6BrN3O5
- Peso molecular:268.02
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Anti-Infection Compound Library
HY-L002
-
Apoptosis Compound Library
HY-L003
-
Immunology/Inflammation Compound Library
HY-L007
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Anti-COVID-19 Compound Library
HY-L052
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Blood Cancer Compound Library
HY-L079
-
Antiparasitic Compound library
HY-L082
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Rare Diseases Drug Library
HY-L102
-
Heterocyclic Compound Library
HY-L138
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Anti-Drug-Resistant Compound Library
HY-L169
-
Anti-Hematopathy Compound Library
HY-L171
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) RRx-001
More- Nat Biomed Eng. 2025 Sep;9(9):1547-1556. [Abstract]
- Nat Commun. 2025 Nov 7;16(1):9846. [Abstract]
- Nat Commun. 2025 May 27;16(1):4887. [Abstract]
- Nat Commun. 2023 Nov 11;14(1):7306. [Abstract]
- Mol Cell. 2019 Sep 19;75(6):1147-1160.e5. [Abstract]
- J Exp Clin Cancer Res. 2019 Feb 20;38(1):90. [Abstract]
- Cell Rep Med. 2025 Feb 18;6(2):101966. [Abstract]
- Biomaterials. 2024 Dec:311:122688. [Abstract]
- Acta Biomater. 2025 Mar 1:194:305-322. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Apr 2;121(14):e2321611121. [Abstract]
- Antioxidants (Basel). 2023 Nov 21;12(12):2024. [Abstract]
- J Med Chem. 2022 Nov 10;65(21):14832-14842. [Abstract]
- J Virol. 2023 Mar 30;97(3):e0001623. [Abstract]
- J Mol Neurosci. 2025 May 9;75(2):65. [Abstract]
- Patent. US20240325538A1.
- Columbia University. 2024 Jun 26.
- Patent. US20240238271A1.
- Patent. US20230226111A1.
- bioRxiv. 2023 Jun 1:2023.06.01.543248. [Abstract]
- Biomed Pharmacother. 2021 Oct:142:111652. [Abstract]
Customer Validation & Images
-
WB
-
WB
-
WB
Ver todos los productos específicos de isoformas Parasite
More
Actividad biológica
|
Plasmodium |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A498 | IC50 |
4.9 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human A498 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human A498 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| A549 | IC50 |
6 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human A549 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| HT-29 | IC50 |
3.4 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| IMR-32 | IC50 |
5.1 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| M21 | IC50 |
2.6 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human M21 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human M21 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| MCF7 | IC50 |
4 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| PANC-1 | IC50 |
2.3 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| RKO | IC50 |
3 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human RKO cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human RKO cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| SCC-7 | IC50 |
1.8 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against mouse SCC-7 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against mouse SCC-7 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| SNB-75 | IC50 |
3.8 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| U-87MG ATCC | IC50 |
2.7 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human U87 cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human U87 cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
| UMSCC22B | IC50 |
2.3 pM
Compound: RRx-001; ABDNAZ
|
Antiproliferative activity against human UMSCC22B cells assessed as cell growth inhibition by CCK8 assay
Antiproliferative activity against human UMSCC22B cells assessed as cell growth inhibition by CCK8 assay
|
[PMID: 34043360] |
RRx-001 (0-5 μM, 24 hours) inhibits MM cells growth and overcomes resistance to novel and conventional therapies[1].
RRx-001 blocks migration of MM cells and associated angiogenesis[1].
RRx-001 induces significant G1 phase growth arrest, with a concomitant decrease in the S phase. RRx-001 triggers significant apoptosis in MM cells[1].
RRx-001 inhibits DNA methylation by downregulating DNA methytransferases[1].
RRx-001 and the supernatant of RRx-001-treated macrophages downregulates CD47 on tumor cells and SIRPα on macrophages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human MM-cell lines (MM.1S, RPMI-8226, H929, ARP1, KMS-11, OPM2, LR5, ANBL6.WT), along with drug resistant cell lines such as (MM.1R, Dox40, LR5, ANBL6.BR, RPMI-8226).
-
Concentration:0-5 μM.
-
Incubation Time:24 hours.
-
Result:Induced a dose-dependent significant (p < 0.05) decrease in viability of all cell lines.
RRx-001 (10 mg/kg, IP, twice a week and once a day) exhibits potent anti-cancer activity on the A549 lung cancer model dependent on the presence of tumor-associated macrophages (TAMs) in tumor tissue[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:CB-17 SCID-mice were subcutaneously inoculated with 5.0 × 106 MM.1S cells in 100 µL of serum-free RPMI 1640 medium[1].
-
Dosage:5 mg/kg or 10 mg/kg.
-
Administration:I.V., thrice-weekly for 24 days.
-
Result:Blocked MM tumor growth and enhances survival.
Treatment was well tolerated, suggested by no apparent weight loss.
-
Animal Model:Female BALB/c nude mice (19.2 ± 1.7 g) based on A549 lung cancer model[2].
-
Dosage:10 mg/kg.
-
Administration:IP, twice a week and once a day.
-
Result:Resulted in the most significant tumor growth retardation.
Reduction of resident macrophages in tumor-bearing mice attenuates the antitumor activity of RRx-001.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 925206-65-1
-
Appearance Solid
-
Peso molecular 268.02
-
Fòrmula C5H6BrN3O5
-
Color White to off-white
-
SMILES
BrCC(N1CC([N+]([O-])=O)([N+]([O-])=O)C1)=O
-
Synonyms
Nibrozetone
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (20)
-
Journal Impact Factor
-
Most Recent
-
Nat Biomed Eng
A live bacteria enzyme assay for identification of human disease mutations and drug screening. [Abstract]2025 Sep;9(9):1547-1556. PMID: 40307426 -
Nat Commun
2025 Nov 7;16(1):9846. PMID: 41203610 -
Nat Commun
Clustering of NLRP3 induced by membrane or protein scaffolds promotes inflammasome assembly. [Abstract]2025 May 27;16(1):4887. PMID: 40425567 -
Nat Commun
Nanomedicine-based co-delivery of a calcium channel inhibitor and a small molecule targeting CD47 for lung cancer immunotherapy. [Abstract]2023 Nov 11;14(1):7306. PMID: 37951973 -
Mol Cell
One-Carbon Metabolism Supports S-Adenosylmethionine and Histone Methylation to Drive Inflammatory Macrophages. [Abstract]2019 Sep 19;75(6):1147-1160.e5. PMID: 31420217 -
J Exp Clin Cancer Res
CCDC6 and USP7 expression levels suggest novel treatment options in high-grade urothelial bladder cancer. [Abstract]2019 Feb 20;38(1):90. PMID: 30786932
RRx-001 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 20;38(1):90. [Abstract]
Protein levels of DNMT1 and CCDC6 in J82 cells treated with different concentrations of RRx-001, as determined by western blot. Vinculin and Tubulin are used as internal controls for sample loading. 5-AZA is used as positive control for inhibition of DNMT1 expression.
RRx-001 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 20;38(1):90. [Abstract]
Whole cell lysates from J82 shCCDC6 or shCTRL cells, treated with different concentrations of RRx-001, or untreated, are immunoblotted with anti-CCDC6 antibody. γH2AX levels are shown. Tubulin is used as loading control.
-
Cell Rep Med
KRASG12D-driven pentose phosphate pathway remodeling imparts a targetable vulnerability synergizing with MRTX1133 for durable remissions in PDAC. [Abstract]2025 Feb 18;6(2):101966. PMID: 39970873 -
Biomaterials
CD40 agonist engineered immunosomes modulated tumor microenvironment and showed pro-immunogenic response, reduced toxicity, and tumor free survival in mice bearing glioblastoma. [Abstract]2024 Dec:311:122688. PMID: 38943821 -
Acta Biomater
Promotion of triple negative breast cancer immunotherapy by combining bioactive radicals with immune checkpoint blockade. [Abstract]2025 Mar 1:194:305-322. PMID: 39805523 -
Proc Natl Acad Sci U S A
NSUN5/TET2-directed chromatin-associated RNA modification of 5-methylcytosine to 5-hydroxymethylcytosine governs glioma immune evasion. [Abstract]2024 Apr 2;121(14):e2321611121. PMID: 38547058 -
Antioxidants (Basel)
Investigation of a UPR-Related Gene Signature Identifies the Pro-Fibrotic Effects of Thrombospondin-1 by Activating CD47/ROS/Endoplasmic Reticulum Stress Pathway in Lung Fibroblasts. [Abstract]2023 Nov 21;12(12):2024. PMID: 38136144 -
J Med Chem
Enhanced Immunotherapy Based on Combining the Pro-phagocytosis and Anti-phagocytosis Checkpoint Blockade for Tumor Eradication. [Abstract]2022 Nov 10;65(21):14832-14842. PMID: 36260348 -
J Virol
Newcastle Disease Virus Manipulates Mitochondrial MTHFD2-Mediated Nucleotide Metabolism for Virus Replication. [Abstract]2023 Mar 30;97(3):e0001623. PMID: 36794935
RRx-001 purchased from MedChemExpress. Usage Cited in: J Virol. 2023 Mar 30;97(3):e0001623. [Abstract]
RRx-001 (2.5, 5, 10, 20, 100 µM; 12 h) significantly and dose-dependently reduces Newcastle disease virus (NDV) NP protein expression in NDV-infected cells.
-
J Mol Neurosci
Therapeutic Hypothermia and Recombinant Erythropoietin Mitigate Brain Microvascular Endothelial Cell Dysfunction via Modulating the Pentose Phosphate Pathway. [Abstract]2025 May 9;75(2):65. PMID: 40343581 -
-
-
-
-
bioRxiv
2023 Jun 1:2023.06.01.543248. PMID: 37398499 -
Biomed Pharmacother
Inhibition of Nrf2-mediated glucose metabolism by brusatol synergistically sensitizes acute myeloid leukemia to Ara-C. [Abstract]2021 Oct:142:111652. PMID: 34112534
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (373.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (281 KB)
-
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7311 mL | 18.6553 mL | 37.3106 mL | 93.2766 mL |
| 5 mM | 0.7462 mL | 3.7311 mL | 7.4621 mL | 18.6553 mL | |
| 10 mM | 0.3731 mL | 1.8655 mL | 3.7311 mL | 9.3277 mL | |
| 15 mM | 0.2487 mL | 1.2437 mL | 2.4874 mL | 6.2184 mL | |
| 20 mM | 0.1866 mL | 0.9328 mL | 1.8655 mL | 4.6638 mL | |
| 25 mM | 0.1492 mL | 0.7462 mL | 1.4924 mL | 3.7311 mL | |
| 30 mM | 0.1244 mL | 0.6218 mL | 1.2437 mL | 3.1092 mL | |
| 40 mM | 0.0933 mL | 0.4664 mL | 0.9328 mL | 2.3319 mL | |
| 50 mM | 0.0746 mL | 0.3731 mL | 0.7462 mL | 1.8655 mL | |
| 60 mM | 0.0622 mL | 0.3109 mL | 0.6218 mL | 1.5546 mL | |
| 80 mM | 0.0466 mL | 0.2332 mL | 0.4664 mL | 1.1660 mL | |
| 100 mM | 0.0373 mL | 0.1866 mL | 0.3731 mL | 0.9328 mL |
RRx-001 Related Classifications
HY-16438 Related Classifications
Powered by Bioz