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Purity: ≥98%
Valspodar (PSC833; SDZ-PSC 833; PSC-833), a cyclosporin-A analog, is a potent and selective inhibitor/modulator of P-glycoprotein (P-gp or MDR-1, an efflux transporter) being investigated as a potential anti-cancer drug and chemosensitizer. It inhibits P-gp-mediated multidrug-resistance (MDR). Valspodar inhibits p-glycoprotein, the multidrug resistance efflux pump, thereby restoring the retention and activity of some drugs in some drug-resistant tumor cells. This agent also induces caspase-mediated apoptosis and has been shown to reverse resistance to several cytotoxic drugs including mitoxantrone and doxorubicin (resistance factors).
| ln Vitro |
Up to 0.75 μg/mL, valspodar (PSC 833) exhibits no cytotoxic effects. When valspodar (0.25, 0.5, and 0.75 μg/mL) is given in addition to DOX-L, the MDR cell type's cell-kill effectiveness increases noticeably. The most lethal combination of DOX and valspodar (0.5 and 0.75 μg/mL) kills almost 70% of the resistant cells[1]. When PSC833 is pretreated, the IC50 value of NSC 279836 in MDA-MB-435mdr cells is reduced to 0.4±0.02 μM in MDR cells, virtually reversing the resistance of MDR cells to NSC 279836[3].
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| ln Vivo |
Valspodar (10 mg/kg, op) has a low mean blood-to-plasma ratio of roughly 0.52 which indicates that it shows negligible blood-cell partitioning. Valspodar exhibits a significant volume of distribution and delayed clearance. Comparable to its structural homolog CsA, valspodar exhibits broad distribution and low hepatic extraction[2]. When PSC833 is preadministered to mice, the NSC 279836 fluorescence intensity in MDR tumors is increased to 94% of that in tumors of the wild type[3].
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| References |
[1]. Bajelan E, et al. Co-delivery of NSC 123127 and PSC 833 (Valspodar) by stealth nanoliposomes for efficient overcoming of multidrug resistance. J Pharm Pharm Sci. 2012 Sep;15(4):568-82.
[2]. PermissionsZ., et al. Pharmacokinetics of PSC 833 (valspodar) in its Cremophor EL formulation in rat.2010,40(1):55-61. [3]. Fei Shen, et al. Dynamic Assessment of NSC 279836 Resistance and Modulation of Multidrug Resistance by Valspodar (PSC833) in Multidrug Resistance Human Cancer Cells. JPET August 2009,330 (2): 423-429 |
| Molecular Formula |
C63H111N11O12
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|---|---|
| Molecular Weight |
1214.62
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| CAS # |
121584-18-7
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| Related CAS # |
121584-18-7
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| SMILES |
O=C([C@H](C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@H](CC(C)C)N(C)C([C@H](C(C)C)NC([C@H](CC(C)C)N(C)C(CN(C)C([C@H](C(C)C)N1)=O)=O)=O)=O)=O)=O)=O)=O)=O)N(C)[C@@H](C([C@H](C)C/C=C/C)=O)C1=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~82.33 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8233 mL | 4.1165 mL | 8.2330 mL | |
| 5 mM | 0.1647 mL | 0.8233 mL | 1.6466 mL | |
| 10 mM | 0.0823 mL | 0.4117 mL | 0.8233 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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