2. Immunology/Inflammation Apoptosis Anti-infection
  3. CD47 Apoptosis Parasite
  4. RRx-001

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

RRx-001 Chemical Structure

CAS No. : 925206-65-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 158 In-stock
Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Solid
1 mg USD 48 In-stock
5 mg USD 144 In-stock
10 mg USD 190 In-stock
50 mg USD 620 In-stock
100 mg USD 990 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 15 publication(s) in Google Scholar

RRx-001 Related Antibodies

Top Publications Citing Use of Products

    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

     

    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.

    RRx-001 Related Antibodies

    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.
    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
    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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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
    References

    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
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    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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