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Submit ReviewPSC 833
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)
Biological Activity for PSC 833
PSC 833 is a 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 for PSC 833
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PSC 833
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 2 | 2 |
Preparing Stock Solutions for PSC 833
The following data is based on the product molecular weight 1214.62. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.02 mM | 41.17 mL | 205.83 mL | 411.65 mL |
| 0.1 mM | 8.23 mL | 41.17 mL | 82.33 mL |
| 0.2 mM | 4.12 mL | 20.58 mL | 41.17 mL |
| 1 mM | 0.82 mL | 4.12 mL | 8.23 mL |
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Product Datasheets for PSC 833
References for PSC 833
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 mitoxan. 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: PSC 833, PSC 833 supplier, PSC833, P-glycoprotein, inhibitors, inhibits, P-gp, cyclosporin, A, analog, analogue, ABCB1, Valspodar, Multidrug, Transporters, 4042, Tocris Bioscience
8 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
Michael et al (2022) Adult human kidney organoids originate from CD24+ cells and represent an advanced model for adult polycystic kidney disease. Nat Genet 54 1690-1701 PMID: 36303074
Slosky et al (2013) Acetaminophen modulates P-glycoprotein functional expression at the blood-brain barrier by a constitutive androstane receptor-dependent mechanism. Mol Pharmacol 84 774 PMID: 24019224
Elbaradie et al (2013) Sex-specific response of rat costochondral cartilage growth plate chondrocytes to 17β-OE involves differential regulation of plasma membrane associated estrogen receptors. Sci Rep 1833 1165 PMID: 23305904
Mark C et al (2021) Biomaterial screening of protein coatings and peptide additives: towards a simple synthetic mimic of a complex natural coating for a bio-artificial kidney. Biomater Sci 9 2209-2220 PMID: 33506836
Jos et al (2021) Implementation of a Human Renal Proximal Tubule on a Chip for Nephrotoxicity and Drug Interaction Studies. J Pharm Sci 110 1601-1614 PMID: 33545187
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
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
Do you know of a great paper that uses PSC 833 from Tocris? Please let us know.
Reviews for PSC 833
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Highly stable.
By
Anonymous on 05/09/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Human brain endothelial cell
50 mg/kg of PSC833 for 15 minutes
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