1. Apoptosis Anti-infection
  2. Apoptosis Parasite
  3. RRx-001

RRx-001 

Cat. No.: HY-16438 Purity: 99.16%
COA Handling Instructions

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
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 158 In-stock
Solid
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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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    RRx-001 purchased from MCE. 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 MCE. 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 MCE. 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.
    • 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].

    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 × 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

    Appearance

    Solid

    Formula

    C5H6BrN3O5

    CAS No.
    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)

    *"≥" 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
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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.

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    Product Name:
    RRx-001
    Cat. No.:
    HY-16438
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