Valspodar | CAS:121584-18-7

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Name:Valspodar; PSC 833
Cat. No. :CS-1074
CAS No. :121584-18-7
Formula:C63H111N11O12
M. Wt. : 1214.62
Solubility:DMSO: 12 mg/mL

Valspodar is a P-glycoprotein (P-gp) inhibitor widely used as overcoming multidrug resistance modulator. 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[1]. 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[3]. 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[2]. Preadministration of PSC833 to mice increases mitoxantrone fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors[3].

PermissionsZ., et al. Pharmacokinetics of PSC 833 (valspodar) in its Cremophor EL formulation in rat.2010,40(1):55-61. Bajelan E, et al. Co-delivery of doxorubicin and PSC 833 (Valspodar) by stealth nanoliposomes for efficient overcoming of multidrug resistance. J Pharm Pharm Sci. 2012 Sep;15(4):568-82. Fei Shen, et al. Dynamic Assessment of Mitoxantrone Resistance and Modulation of Multidrug Resistance by Valspodar (PSC833) in Multidrug Resistance Human Cancer Cells. JPET August 2009,330 (2): 423-429