Valspodar
Based on 17 publication(s) in Google Scholar
Valspodar (PSC 833) is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.0%
- CAS No.: 121584-18-7
- Formule: C63H111N11O12
- Masse moléculaire:1214.62
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Valspodar
More- Exploration. 2026 May 28;6(3):20240134. [Abstract]
- Food Chem. 2021 May 1;343:128510. [Abstract]
- Cell Death Discov. 2024 Aug 14;10(1):364. [Abstract]
- Cell Prolif. 2022 Mar;55(3):e13190. [Abstract]
- Front Pharmacol. 2019 Jun 26:10:722. [Abstract]
- Hepatol Commun. 2024 May 2;8(5):e0437. [Abstract]
- FASEB J. 2019 Feb;33(2):2084-2094. [Abstract]
- Transl Oncol. 2021 Jan;14(1):100917. [Abstract]
- Antiviral Res. 2021 Sep:193:105124. [Abstract]
- J Biol Chem. 2022 Apr;298(4):101756. [Abstract]
- Sci Rep. 2017 Dec 22;7(1):18069. [Abstract]
- J Drug Target. 2016;24(5):441-9. [Abstract]
- Drug Metab Pharmacokinet. 2022 Feb:42:100430. [Abstract]
- Lasers Surg Med. 2017 Sep;49(7):719-726. [Abstract]
- J Asian Nat Prod Res. 2020 Jul 1;1-14. [Abstract]
- bioRxiv. 2023 Feb 23:2023.02.23.529736. [Abstract]
- Oncotarget. 2016 Oct 18;7(42):68623-68637. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
Activité biologique
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | IC50 |
0.11 μM
Compound: PSC-833 (Valspodar)
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TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
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[PMID: 10820137] |
| L929 | IC50 |
>100 μM
Compound: 3
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Cytotoxicity against mouse L929 cells after 72 hrs
Cytotoxicity against mouse L929 cells after 72 hrs
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[PMID: 22320402] |
| LLC-PK1 | IC50 |
0.0222 μM
Compound: PSC-833 (Valspodar)
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TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 10997946] |
| LLC-PK1 | IC50 |
0.291 μM
Compound: PSC-833 (Valspodar)
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TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical) (Doxorubicin: 0.8 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical) (Doxorubicin: 0.8 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 9914792] |
| LLC-PK1 | IC50 |
1.06 μM
Compound: PSC-833 (Valspodar)
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TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical) (Vinblastine: 0.1 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Vinblastine transepithelial transport (basal to apical) (Vinblastine: 0.1 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 9914792] |
| SW-620 | IC50 |
0.1 μM
Compound: PSC833
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Reversal of P-gp-mediated resistance to doxorubicin in human SW620 cells assessed as reduction in doxorubin IC50 at 400 nM after 72 hrs by SRB assay
Reversal of P-gp-mediated resistance to doxorubicin in human SW620 cells assessed as reduction in doxorubin IC50 at 400 nM after 72 hrs by SRB assay
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[PMID: 25215856] |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 121584-18-7
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Appearance Solid
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Masse moléculaire 1214.62
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Formule C63H111N11O12
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Color White to yellow
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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
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Synonyms
PSC 833
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (17)
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Journal Impact Factor
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Most Recent
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Exploration
Tumor-Mimic Artificial Cell Integrated With In Situ Synthetic Biology for Testing of Antitumor Drug Sensitivity. [Abstract]2026 May 28;6(3):20240134. PMID: 42382689 -
Food Chem
2021 May 1;343:128510. PMID: 33172753 -
Cell Death Discov
Generation of a conditional cellular senescence model using proximal tubule cells and fibroblasts from human kidneys. [Abstract]2024 Aug 14;10(1):364. PMID: 39143064 -
Cell Prolif
Functional differentiation and scalable production of renal proximal tubular epithelial cells from human pluripotent stem cells in a dynamic culture system. [Abstract]2022 Mar;55(3):e13190. PMID: 35102634 -
Front Pharmacol
A Danshensu-Tetramethylpyrazine Conjugate DT-010 Overcomes Multidrug Resistance in Human Breast Cancer. [Abstract]2019 Jun 26:10:722. PMID: 31293428 -
Hepatol Commun
Inhibition of the transmembrane transporter ABCB1 overcomes resistance to doxorubicin in patient-derived organoid models of HCC. [Abstract]2024 May 2;8(5):e0437. PMID: 38696353 -
FASEB J
ABCB1 (P-glycoprotein) regulates vitamin D absorption and contributes to its transintestinal efflux. [Abstract]2019 Feb;33(2):2084-2094. PMID: 30222077 -
Transl Oncol
Cross-resistance of cisplatin selected cells to anti-microtubule agents: Role of general survival mechanisms. [Abstract]2021 Jan;14(1):100917. PMID: 33129114 -
Antiviral Res
2021 Sep:193:105124. PMID: 34197862 -
J Biol Chem
The naturally occurring flavonoid nobiletin reverses methotrexate resistance via inhibition of P-glycoprotein synthesis. [Abstract]2022 Apr;298(4):101756. PMID: 35202652 -
Sci Rep
LUCS (Light-Up Cell System), a universal high throughput assay for homeostasis evaluation in live cells. [Abstract]2017 Dec 22;7(1):18069. PMID: 29273711 -
J Drug Target
2016;24(5):441-9. PMID: 26373825
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.
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Drug Metab Pharmacokinet
Investigation of the role and quantitative impact of breast cancer resistance protein on drug distribution into brain and CSF in rats. [Abstract]2022 Feb:42:100430. PMID: 34896751 -
Lasers Surg Med
The sensitivity of glioma cells to pyropheophorbide-αmethyl ester-mediated photodynamic therapy is enhanced by inhibiting ABCG2. [Abstract]2017 Sep;49(7):719-726. PMID: 28370217 -
J Asian Nat Prod Res
Cycloastragenol inhibits Aβ1-42-induced blood-brain barrier disruption and enhances soluble Aβ efflux in vitro. [Abstract]2020 Jul 1;1-14. PMID: 32608254 -
bioRxiv
The Multidrug Resistance Transporter P-glycoprotein Confers Resistance to Ferroptosis Inducers. [Abstract]2023 Feb 23:2023.02.23.529736. PMID: 36945397 -
Oncotarget
DCTPP1 attenuates the sensitivity of human gastric cancer cells to 5-fluorouracil by up-regulating MDR1 expression epigenetically. [Abstract]2016 Oct 18;7(42):68623-68637. PMID: 27612427
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.
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (289 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| 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 |
Valspodar Related Classifications
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