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

RRx-001 

Cat. No.: HY-16438 Purity: 99.82%
Handling Instructions

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. 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 (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1560 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    RRx-001 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 20;38(1):90.

    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 MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 20;38(1):90.

    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.
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    Description

    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].

    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].

    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

    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 provided by MCE.
    References
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    Product Name:
    RRx-001
    Cat. No.:
    HY-16438
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