PSC 833

Pricing Availability Delivery Time Qty
Cat.No. 4042 - PSC 833 | C63H111N11O12 | CAS No. 121584-18-7
Description: Inhibitor of P-gp-mediated MDR
Alternative Names: Valspodar
Chemical Name: 6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoic acid]-7-L-valine-cyclosporin A
Purity: ≥98% (HPLC)
Datasheet
Citations (4)
Reviews
Literature

Biological Activity

P-glycoprotein (P-gp) modulator; inhibits P-gp-mediated multidrug-resistance (MDR). Reverses resistance to several cytotoxic drugs including mitoxantrone and doxorubicin (resistance factors are 2.0 and 6.5 respectively) in human MDR cancer cell lines. Non-immunosuppressive analog of cyclosporin A (Cat. No. 1101).

Technical Data

M. Wt 1214.62
Formula C63H111N11O12
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 121584-18-7
PubChem ID 5281884
InChI Key YJDYDFNKCBANTM-QCWCSKBGSA-N
Smiles C[C@H](C)[C@@H](C1=O)NC([C@H](CC(C)C)N(C(CN(C([C@H]([C@H](C)C)NC([C@H]([C@]([C@H](C)C/C=C/C)=O)N(C([C@H]([C@@H](C)C)N(C([C@H](CC(C)C)N(C([C@H](CC(C)C)N(C([C@@H](C)NC([C@H](C)NC([C@H](CC(C)C)N1C)=O)=O)=O)C)=O)C)=O)C)=O)C)=O)=O)C)=O)C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 4.86 4

Preparing Stock Solutions

The following data is based on the product molecular weight 1214.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.82 mL 4.12 mL 8.23 mL
5 mM 0.16 mL 0.82 mL 1.65 mL
10 mM 0.08 mL 0.41 mL 0.82 mL
50 mM 0.02 mL 0.08 mL 0.16 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

Song et al (1998) Modulation of the tumor disposition of vinca alkaloids by PSC 833 in vitro and in vivo. J.Pharmacol.Exp.Ther. 287 963 PMID: 9864280

Goda et al (2007) Complete inhibition of P-glycoprotein by simulataneous treatment with a distinct class of modulators and the UIC2 monoclonal antibody. J.Pharmacol.Exp.Ther. 320 81 PMID: 17050779

Shen et al (2008) Quantitation of doxorubicine uptake, efflux, and modulation of multidrug resistance (MDR) in MDR human cancer cells. J.Pharmacol.Exp.Ther. 324 95 PMID: 17947497

Shen et al (2009) Dynamic assessment of mitoxantrone resistance and modulation of multidrug resistance by Valspodar (PSC833) in multidrug resistance human cancer cells. J.Pharmacol.Exp.Ther. 330 423 PMID: 19423841


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Keywords: PSC 833, PSC 833 supplier, PSC833, P-glycoprotein, inhibitors, inhibits, P-gp, cyclosporin, A, analog, analogue, ABCB1, Valspodar, Multidrug, Transporters, 4042, Tocris Bioscience

4 Citations for PSC 833

Citations are publications that use Tocris products. Selected citations for PSC 833 include:

Lipka et al (2012) Intracellular retention of ABL kinase inhibitors determines commitment to apoptosis in CML cells. PLoS One 7 e40853 PMID: 22815843

Ong et al (2013) Ciprofloxacin is actively transported across bronchial lung epithelial cells using a Calu-3 air interface cell model. Antimicrob Agents Chemother 57 2535 PMID: 23507281

Elbaradie et al (2013) Sex-specific response of rat costochondral cartilage growth plate chondrocytes to 17β-estradiol involves differential regulation of plasma membrane associated estrogen receptors. Sci Rep 1833 1165 PMID: 23305904

Kim and Bynoe (2016) A2A adenosine receptor modulates drug efflux transporter P-glycoprotein at the blood-brain barrier. J Clin Invest 126 1717 PMID: 27043281


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Literature in this Area

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