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[CAS NO. 925206-65-1] RRx-001
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-16438 |
| Brand: | MCE |
| CAS: | 925206-65-1 |
Overview
| MDL | MFCD25976849 |
|---|---|
| Molecular Weight | 268.02 |
| Molecular Formula | C5H6BrN3O5 |
| SMILES | BrCC(N1CC([N+]([O-])=O)([N+]([O-])=O)C1)=O |
4 Publications Citing Use of MCE
Summary
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug 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] .
In Vitro
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 concomitant decrease in 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| 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. |
In Vivo
RRx-001 (5 mg/kg or 10 mg/kg, I.V., thrice-weekly for 24 days) inhibits tumor growth and prolongs survival in a xenograft mouse model
[1]
.
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]
.
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 × 10 6 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. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04525014 | EpicentRx, Inc.|Texas Children´s Cancer Center |
Brain Tumor, Recurrent|Brain Tumor, Pediatric|Central Nervous System Neoplasms|Unspecified Childhood Solid Tumor, Protocol Specific
|
December 1, 2022 | Phase 1 |
| NCT02801097 | EpicentRx, Inc. |
Malignant Solid Tumor|Metastatic Cancer|Advanced Cancer
|
August 30, 2016 | Phase 1 |
| NCT03699956 | EpicentRx, Inc. |
Carcinoma, Small Cell Lung
|
December 24, 2018 | Phase 3 |
| NCT02215512 | EpicentRx, Inc. |
Brain Metastases
|
February 6, 2015 | Phase 1 |
| NCT02489903 | EpicentRx, Inc. |
Small Cell Carcinoma|Carcinoma, Non-Small-Cell Lung|Neuroendocrine Tumors|Ovarian Epithelial Cancer
|
June 2015 | Phase 2 |
| NCT02871843 | EpicentRx, Inc. |
Glioblastoma|Oligodendroglioma|Anaplastic Oligodendroglioma
|
February 14, 2017 | Phase 1 |
| NCT02096354 | EpicentRx, Inc. |
Colorectal Neoplasms
|
May 2014 | Phase 2 |
| NCT02452970 | EpicentRx, Inc. |
Cholangiocarcinoma
|
July 16, 2015 | Phase 2 |
| NCT02096341 | EpicentRx, Inc. |
Malignant Solid Tumor|Lymphomas
|
April 2014 | Phase 1 |
| NCT03515538 | EpicentRx, Inc.|Prothex Pharma, Inc. |
Oral Mucositis
|
July 12, 2018 | Phase 2 |
| NCT01359982 | EpicentRx, Inc. |
Malignant Solid Tumor|Lymphomas
|
September 2011 | Phase 1 |
| NCT05566041 | EpicentRx, Inc.|Sciclone Pharmaceuticals (China) Co., Ltd. |
Carcinoma, Small Cell Lung
|
August 1, 2022 | Phase 3 |
| NCT02518958 | EpicentRx, Inc. |
Malignant Solid Tumor|Lymphoma
|
July 21, 2015 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 373.11 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.7311 mL | 18.6553 mL | 37.3107 mL |
| 5 mM | 0.7462 mL | 3.7311 mL | 7.4621 mL |
| 10 mM | 0.3731 mL | 1.8655 mL | 3.7311 mL |
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.
- [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.
- [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.
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