Art. -Nr.: HY-17384

Valspodar

(Synonyms: PSC 833)

17 Cited Publications

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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.

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Reinheit: 98.0%
CAS. Nr.: 121584-18-7
Formel: C₆₃H₁₁₁N₁₁O₁₂
Molecular Weight:1214.62

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Valspodar Chemical Structure

CAS. Nr.: 121584-18-7

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	0.11 μM Compound: PSC-833 (Valspodar)	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	[PMID: 10820137]
L929	IC₅₀	>100 μM Compound: 3	Cytotoxicity against mouse L929 cells after 72 hrs Cytotoxicity against mouse L929 cells after 72 hrs	[PMID: 22320402]
LLC-PK1	IC₅₀	0.0222 μM Compound: PSC-833 (Valspodar)	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	[PMID: 10997946]
LLC-PK1	IC₅₀	0.291 μM Compound: PSC-833 (Valspodar)	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	[PMID: 9914792]
LLC-PK1	IC₅₀	1.06 μM Compound: PSC-833 (Valspodar)	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	[PMID: 9914792]
SW-620	IC₅₀	0.1 μM Compound: PSC833	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	[PMID: 25215856]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 121584-18-7
Appearance Solid
Molecular Weight 1214.62
Formel C₆₃H₁₁₁N₁₁O₁₂
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
Synonyms

PSC 833
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (17)

All Cell Proliferation/Viability Assay

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Journal Impact Factor

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

P-glycoprotein (ABCB1) is involved in vitamin K efflux. [Abstract]

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

Valspodar limits human cytomegalovirus infection and dissemination. [Abstract]

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

Raloxifene nanomicelles reduce the growth of castrate-resistant prostate cancer. [Abstract]

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.
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.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.8233 mL

4.1165 mL

8.2330 mL

5 mM

0.1647 mL

0.8233 mL

1.6466 mL

10 mM

0.0823 mL

0.4117 mL

0.8233 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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.

MedChemExpress (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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Bajelan E, et al. Co-delivery of NSC 123127 and PSC 833 (Valspodar) by stealth nanoliposomes for efficient overcoming of multidrug resistance. J Pharm Pharm Sci. 2012 Sep;15(4):568-82. [Content Brief]

[2]. PermissionsZ., et al. Pharmacokinetics of PSC 833 (valspodar) in its Cremophor EL formulation in rat.2010,40(1):55-61.

[3]. Fei Shen, et al. Dynamic Assessment of NSC 279836 Resistance and Modulation of Multidrug Resistance by Valspodar (PSC833) in Multidrug Resistance Human Cancer Cells. JPET August 2009,330 (2): 423-429

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Valspodar

17 Cited Publications

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Valspodar

Peptidomimetic Library

Macrocyclic Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Valspodar

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Valspodar

Peptidomimetic Library

Macrocyclic Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Valspodar

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Valspodar Related Classifications

HY-17384 Related Classifications