产品信息
抗原名称
P-glycoprotein
商品描述
Valspodar (PSC 833) is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.
分子量
1214.62
纯度
98%
可溶性
DMSO : 12 mg/mL (9.88 mM; Need ultrasonic and warming)
外观
white to beige powder
In vitro(体外研究)
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. 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.
In vivo(体内研究)
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. Preadministration of PSC833 to mice increases mitoxantrone fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors.
背景
别名
伐司朴达
分子式
C63H111N11O12
CAS号
121584-18-7
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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