Valspodar

SKU: orb1706487

Description

Valspodar (PSC 833) is a potent and specific inhibitor of P-glycoprotein, functioning as a multidrug resistance (MDR) modulator. It is widely utilized in oncology research, particularly in both in vitro and in vivo studies of advanced epithelial ovarian cancer, to investigate chemosensitization and overcome drug resistance.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 121584-18-7
• MW: 1214.62
• Purity: >99.99% (May vary between batches)
• Formula: C₆₃H₁₁₁N₁₁O₁₂
• SMILES: C\C=C\C[C@@H](C)C(=O)[C@@H]1N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C(=O)[C@@H](NC1=O)C(C)C)C(C)C
• Target: P-gp
• Solubility: DMSO:90 mg/mL (74.1 mM);10% DMSO+90% Corn Oil:3.3 mg/mL (2.72 mM)

Bioactivity

• Target IC50:
  MDR cells:0.4 μM|L929 cells:> 100 μM|SW620 cells:0.1 μM
• 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 . Preadministration of PSC833 to mice increases NSC 279836 fluorescent intensity in MDR tumors to 94% of that observed in wild-type tumors .
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• 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 . 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Pgp, P-glycoprotein, PSC 833, PSC833, PSC-833, Valspodar

Compound Identifiers

PubChem CID

5281884