RRx-001

Name: RRx-001
Brand: MedChemExpress
SKU: HY-16438
Rating: 5.0 (16 reviews)

Cat. No.: HY-16438 Purity: 99.16%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

RRx-001 Chemical Structure

CAS No. : 925206-65-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 158	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 158	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 620	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 16 publication(s) in Google Scholar

13 Publications Citing Use of MCE RRx-001

: RRx-001 purchased from MedChemExpress. Usage Cited in: J Virol. 2023 Feb 16;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.

: 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.

: 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.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

IC₅₀ & Target

Plasmodium

Cellular Effect

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	6.00 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	4.00 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	3.00 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]

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 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 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].

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.

Clinical Trial

Molecular Weight

268.02

Formula

C₅H₆BrN₃O₅

CAS No.

925206-65-1

Appearance

Solid

Color

White to off-white

SMILES

BrCC(N1CC([N+]([O-])=O)([N+]([O-])=O)C1)=O

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

In Vitro:

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.

Preparing
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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.16%

Select Batch:

Data Sheet (282 KB) SDS (584 KB)

COA (251 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

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. [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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RRx-001925206-65-1RRx001RRx 001CD47ApoptosisParasiteCluster of Differentiation 47MER6OA3Inhibitorinhibitorinhibit

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RRx-001

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13 Publications Citing Use of MCE RRx-001

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RRx-001 Related Classifications

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