1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. Valspodar

Valspodar  (Synonyms: PSC 833)

Cat. No.: HY-17384 Purity: ≥98.0%
COA Handling Instructions

Valspodar (PSC 833) is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.

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

Valspodar Chemical Structure

Valspodar Chemical Structure

CAS No. : 121584-18-7

Size Price Stock Quantity
1 mg USD 350 In-stock
5 mg USD 1120 In-stock
10 mg USD 1800 In-stock
25 mg USD 2880 In-stock
50 mg USD 4600 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 18 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Valspodar purchased from MedChemExpress. Usage Cited in: J Drug Target. 2016;24(5):441-9.  [Abstract]

    Cells are co-treated with 5 μM of free LY156758 or an equivalent dose of SMA-LY156758 and either vehicle control (0.01% DMSO), Elacridar (1 μM), KO143 (5 μM), Valspodar (1 μM) or a combination of efflux inhibitors for 6 h.

    Valspodar purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Oct 18;7(42):68623-68637.  [Abstract]

    The effect of MDR1 on drug sensitivity to 5-FU in BGC-823 cells is tested by using MDR1 specific inhibitor PSC833. Cells are exposed to 2 μM 5-FU combined with PSC833 (0, 1, 3, 9 μM) for 72 h. Cell viability is detected by CCK-8 assay.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Valspodar (PSC 833) is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.

    In Vitro

    Valspodar (PSC 833) has no cytotoxicity effects at up to the concentration of 0.75 μg/mL. Valspodar (0.25, 0.5 and 0.75 μg/mL) and DOX-L are added to the DOX resistant cells, and cell kill efficacy of MDR cell type increases significantly when valspodar is administered alongside DOX-L. Valspodar (0.5 and 0.75 μg/mL), in combination with all concentrations of DOX, are most toxic and kill more than 70% of the resistant cells[1].
    Pretreatment with PSC833 decreases the IC50 value of NSC 279836 in MDA-MB-435mdr cells to 0.4±0.02 μM in MDR cells and almost completely reverses the resistance of MDR cells to NSC 279836[3].

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

    In Vivo

    valspodar (10 mg/kg, o.p.) exhibits minimal blood-cell partitioning as reflected in its low mean blood-to-plasma ratio of approximately 0.52. Valspodar displays properties of slow clearance and a large volume of distribution. Valspodar shows properties of low hepatic extraction and wide distribution, similar to that of its structural analogue CsA[2].
    Preadministration of PSC833 to mice increases NSC 279836 fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors[3].

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

    Clinical Trial
    Molecular Weight

    1214.62

    Formula

    C63H111N11O12

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C([C@H](C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@H](CC(C)C)N(C)C([C@H](C(C)C)NC([C@H](CC(C)C)N(C)C(CN(C)C([C@H](C(C)C)N1)=O)=O)=O)=O)=O)=O)=O)=O)=O)N(C)[C@@H](C([C@H](C)C/C=C/C)=O)C1=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (82.33 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 0.8233 mL 4.1165 mL 8.2330 mL
    5 mM 0.1647 mL 0.8233 mL 1.6466 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
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    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

    ×
    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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (2.06 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)

    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

    Purity: 99.27%

    References
    Cell Assay
    [1]

    The in vitro cytotoxicity of various formulations against T47D/TAMR-6 cells is investigated by MTT assay. A 104 T47D/TAMR-6 cells are cultured in 96-well plate containing RPMI medium and incubated overnight to allow cell attachment. After 48 hours incubation, fresh medium containing serial concentration of various drug formulations, including free DOX, DOX-L, mixture of DOX-L and free Valspodar (PSC 833), mixture of DOX-L and PSC-L and DOX/PSC-L are added. The plates are then incubated for an additional 48 hours before washing with normal saline followed by adding MTT solution (0.5 mg/mL) to each well, and incubated for 4 h at 37°C. Then, the medium is removed, and DMSO is added to dissolve the formazan crystals. The plates are mildly shaken for 10 min to ensure the dissolution of formazan. The formazan dye is measured spectrophotometrically using microplate reader at 570 nm with reference standard of 690 nm as described before.

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

    Animal Administration
    [2]

    Male Sprague–Dawley rats (250-350 g) are housed in temperature-controlled rooms with 12 h of light per day. The animals had free access to food and water prior to experimentation. Rats are divided into two groups: one group (n=6) receives intravenous dose (5 mg/kg) of valspodar and the other group administered valspodar orally (10 mg/kg). Stereoselective pharmacokinetics of desbutylhalofantrine, a metabolite of halofantrine, in the rat after administration of the racemic metabolite or parent drug. After surgery, the rats are transferred to their regular holding cages and allowed free access to water, but food is withheld overnight. The next morning, rats are transferred to the metabolic cages and dosed with valspodar.

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

    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 0.8233 mL 4.1165 mL 8.2330 mL 20.5826 mL
    5 mM 0.1647 mL 0.8233 mL 1.6466 mL 4.1165 mL
    10 mM 0.0823 mL 0.4117 mL 0.8233 mL 2.0583 mL
    15 mM 0.0549 mL 0.2744 mL 0.5489 mL 1.3722 mL
    20 mM 0.0412 mL 0.2058 mL 0.4117 mL 1.0291 mL
    25 mM 0.0329 mL 0.1647 mL 0.3293 mL 0.8233 mL
    30 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 mL
    40 mM 0.0206 mL 0.1029 mL 0.2058 mL 0.5146 mL
    50 mM 0.0165 mL 0.0823 mL 0.1647 mL 0.4117 mL
    60 mM 0.0137 mL 0.0686 mL 0.1372 mL 0.3430 mL
    80 mM 0.0103 mL 0.0515 mL 0.1029 mL 0.2573 mL
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    Valspodar 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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