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Valspodar

Cat. No. M6267
Valspodar Structure
Synonym:

PSC 833

Size Price Availability Quantity
5mg USD 200 In stock
10mg USD 350 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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. 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.

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. Preadministration of PSC833 to mice increases mitoxantrone fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors.

Protocol
Cell Experiment
Cell lines T47D/TAMR-6 cells
Preparation method 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.
Concentrations 0.5 mg/mL
Incubation time 48 h
Animal Experiment
Animal models Male Sprague–Dawley rats
Formulation saline
Dosages 10 mg/kg
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 1214.62
Formula C63H111N11O12
CAS Number 121584-18-7
Purity >98%
Solubility 12 mg/mL in DMSO
Storage at -20°C
References

Development of a polymeric micellar formulation for valspodar and assessment of its pharmacokinetics in rat.
Binkhathlan Z, et al. Eur J Pharm Biopharm. 2010 Jun;75(2):90-5.. PMID: 20332028.

Pharmacokinetics of PSC 833 (valspodar) in its Cremophor EL formulation in rat.
Binkhathlan Z, et al. Xenobiotica. 2010 Jan;40(1):55-61. PMID: 19903013.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Valspodar, PSC 833 supplier, P-gp, inhibitors

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