2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. Dofequidar

Dofequidar  (Synonyms: MS-209 free base)

Cat. No.: HY-17013 Purity: 98.17%
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Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect.

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

Dofequidar Chemical Structure

Dofequidar Chemical Structure

CAS No. : 129716-58-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Dofequidar:

Dofequidar Related Antibodies

Top Publications Citing Use of Products

    Dofequidar purchased from MedChemExpress. Usage Cited in: Am J Transl Res. 2020 May 15;12(5):1807-1823.  [Abstract]

    CCK-8 assay showing a significantly lower cisplatin IC50 for the P-gp inhibitor Dofequidar fumarate (5 μM) treatment group compared with the vehicle control group in MG-63 and MNNG/HOS cells.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect[1][2].

    In Vitro

    Dofequidar in the in vitro proliferation and chemosensitivity assays of human small cell lung cancer SBC-3/ADM and SBC-3 cells completely reverses the multidrug resistance of SBC-3/ADM cells to Etoposide (VP-16) (HY-13629), Adriamycin, and Vincristine (HY-N0488) at concentrations of 3-10 μM, with little effect on the sensitivity of SBC-3 cells[1].
    Dofequidar in the P-gp expression analysis experiment of human small cell lung cancer SBC-3/ADM and SBC-3 cells does not change the P-gp expression of SBC-3 cells, while SBC-3/ADM cells express P-gp[1].
    Dofequidar at various concentrations reduces the proportion of side population (SP) cells in a dose-dependent manner in the SP cell sorting experiment of multiple cancer cell lines[2].
    Dofequidar increases the intracellular concentration of ABCC1⁄MDR-associated protein (MRP) in K562/BCRP cells in the intracellular drug accumulation experiment[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Dofequidar Related Antibodies
    In Vivo

    Dofequidar (200 mg/kg; orally administered; starting from days 10 or 14 after tumor cell inoculation, 4 doses) in NK cell-depleted SCID mice inoculated with SBC-3/ADM or SBC-3 cells significantly inhibits the metastasis of SBC-3/ADM cells to multiple organs when combined with Etoposide (VP-16) (HY-13629) or Adriamycin[1].
    Dofequidar (200 mg/kg; orally administered; given 30 minutes before Irinotecan (CPT-11) (HY-16562) injection, and both are administered on days 0, 4, and 8; throughout the experiment) in nude mice inoculated with HeLa SP cells significantly reduces the tumor volume when combined with Irinotecan[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: 6- to 8-week-old male severe combined immunodeficiency (SCID) mice, depleted of natural killer (NK) cells by intraperitoneal injection of TM-β1 Ab (1 mg/mouse) 2 days before tumor inoculation, and then inoculated intravenously with SBC-3 or SBC-3/ADM cells[1]
    Dosage: 200 mg/kg
    Administration: Orally administered; the mice inoculated with SBC-3 cells were treated on days 14, 15, 21, and 22; the mice inoculated with SBC-3/ADM cells were treated on days 10, 11, 17, and 18.
    Result: Combined use with Etoposide (VP-16) (HY-13629) or Adriamycin can significantly inhibit metastasis formation by SBC-3/ADM cells to the liver, kidneys, and lymph nodes, and the weight of the liver of the treated mice was significantly less than that of other groups.
    Animal Model: 5- to 6-week-old female BALB/c-nu/nu (nude) mice, inoculated subcutaneously with HeLa SP cells[2]
    Dosage: 200 mg/kg
    Administration: Orally administered 30 minutes before intravenous injection of Irinotecan (67 mg/kg); on days 0, 4, and 8
    Result: Co-treatment with Irinotecan drastically decreased the tumor volume.
    Clinical Trial
    Molecular Weight

    481.59

    Formula

    C30H31N3O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC(COC1=C2C=CC=NC2=CC=C1)CN3CCN(C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)CC3
    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 : 50 mg/mL (103.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0765 mL 10.3823 mL 20.7646 mL
    5 mM 0.4153 mL 2.0765 mL 4.1529 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.

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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    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 (5.19 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.
    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 2.0765 mL 10.3823 mL 20.7646 mL 51.9114 mL
    5 mM 0.4153 mL 2.0765 mL 4.1529 mL 10.3823 mL
    10 mM 0.2076 mL 1.0382 mL 2.0765 mL 5.1911 mL
    15 mM 0.1384 mL 0.6922 mL 1.3843 mL 3.4608 mL
    20 mM 0.1038 mL 0.5191 mL 1.0382 mL 2.5956 mL
    25 mM 0.0831 mL 0.4153 mL 0.8306 mL 2.0765 mL
    30 mM 0.0692 mL 0.3461 mL 0.6922 mL 1.7304 mL
    40 mM 0.0519 mL 0.2596 mL 0.5191 mL 1.2978 mL
    50 mM 0.0415 mL 0.2076 mL 0.4153 mL 1.0382 mL
    60 mM 0.0346 mL 0.1730 mL 0.3461 mL 0.8652 mL
    80 mM 0.0260 mL 0.1298 mL 0.2596 mL 0.6489 mL
    100 mM 0.0208 mL 0.1038 mL 0.2076 mL 0.5191 mL
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    Dofequidar 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:

    Dofequidar129716-58-1MS-209MS209MS 209P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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