PSC 833
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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References
References are publications that support the products' biological activity.
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
If you know of a relevant reference for PSC 833, please let us know.
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Keywords: PSC833 P-glycoprotein inhibitors inhibits P-gp cyclosporin A analog analogue ABCB1 Valspodar Multidrug Transporters
2 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
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
Do you know of a great paper that uses PSC 833 from Tocris? If so please let us know.