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

Valspodar (Synonyms: PSC 833)

Cat. No.: HY-17384 Purity: 99.27%
Handling Instructions

Valspodar 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
10 mM * 1 mL in DMSO USD 641 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    Cells are co-treated with 5 μM of free Raloxifene or an equivalent dose of SMA-raloxifene 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 MCE. Usage Cited in: Oncotarget. 2016 Oct 18;7(42):68623-68637.

    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 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 mitoxantrone in MDA-MB-435mdr cells to 0.4±0.02 μM in MDR cells and almost completely reverses the resistance of MDR cells to mitoxantrone[3].

    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 cyclosporine A[2]. Preadministration of PSC833 to mice increases mitoxantrone fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors[3].

    Clinical Trial
    Molecular Weight

    1214.62

    Formula

    C₆₃H₁₁₁N₁₁O₁₂

    CAS No.

    121584-18-7

    SMILES

    O=C([[email protected]](C(C)C)N(C)C([[email protected]](CC(C)C)N(C)C([[email protected]](CC(C)C)N(C)C([[email protected]@H](C)NC([[email protected]](C)NC([[email protected]](CC(C)C)N(C)C([[email protected]](C(C)C)NC([[email protected]](CC(C)C)N(C)C(CN(C)C([[email protected]](C(C)C)N1)=O)=O)=O)=O)=O)=O)=O)=O)=O)N(C)[[email protected]@H](C([[email protected]](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 : 12 mg/mL (9.88 mM; Need ultrasonic and warming)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM --- --- ---
    *Please refer to the solubility information to select the appropriate solvent.
    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

    Purity: 99.27%

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