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Valspodar

Catalog No. T17216 CAS 121584-18-7

Synonyms: PSC 833

Valspodar (PSC 833) is a specific P-glycoprotein inhibitor and MDR regulator often used as a chemical sensitizer to study advanced epithelial ovarian cancer.

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Valspodar, CAS 121584-18-7

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10 mg	In stock	$ 1,490.00

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Purity: 95%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Valspodar (PSC 833) is a specific P-glycoprotein inhibitor and MDR regulator often used as a chemical sensitizer to study advanced epithelial ovarian cancer.
Targets&IC50	MDR cells:0.4μM
In vitro	At concentrations up to 0.75 μg/mL, Valspodar (PSC 833) exhibits no cytotoxic effects. When Valspodar (0.25, 0.5, and 0.75 μg/mL) and DOX-L are introduced to DOX-resistant cells, the cell-killing efficacy of the MDR cell type significantly increases, particularly with the administration of Valspodar alongside DOX-L. The combination of Valspodar (0.5 and 0.75 μg/mL) with all concentrations of DOX is the most toxic, resulting in the death of more than 70% of the resistant cells [1]. Pretreatment with PSC833 reduces the IC50 value of NSC 279836 in MDA-MB-435mdr cells to 0.4±0.02 μM and almost completely reverses the resistance of MDR cells to NSC 279836 [2].
In vivo	Administered orally at a dose of 10 mg/kg, Valspodar exhibits minimal blood-cell partitioning, as indicated by its low mean blood-to-plasma ratio of approximately 0.52. Valspodar demonstrates characteristics of slow clearance and a large volume of distribution. Its properties include low hepatic extraction and wide distribution, akin to those observed in its structural analogue CsA [3]. Preadministration of PSC833 to mice increases NSC 279836 fluorescent intensity in MDR tumors to 94% of that observed in wild-type tumors [2].

Synonyms	PSC 833
Molecular Weight	1214.62
Formula	C63H111N11O12
CAS No.	121584-18-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (74.10 mM), Sonication is recommended.

References and Literature

1. Bajelan E, et al. Co-delivery of doxorubicin and PSC 833 (Valspodar) by stealth nanoliposomes for efficient overcoming of multidrug resistance. J Pharm Pharm Sci. 2012 Sep;15(4):568-82. 2. Fei Shen, et al. Dynamic Assessment of Mitoxantrone Resistance and Modulation of Multidrug Resistance by Valspodar (PSC833) in Multidrug Resistance Human Cancer Cells. JPET August 2009,330 (2): 423-429 3. PermissionsZ., et al. Pharmacokinetics of PSC 833 (valspodar) in its Cremophor EL formulation in rat.2010,40(1):55-61.

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Keywords

Valspodar 121584-18-7 Membrane transporter/Ion channel Neuroscience P-gp PSC-833 PSC833 PSC 833 inhibitor inhibit

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