您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Tariquidar dihydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Tariquidar dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tariquidar dihydrochloride图片
CAS NO:1992047-62-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
XR9576 dihydrochloride
产品介绍
Tariquidar dihydrochloride (XR9576 dihydrochloride) 是一种有效的特异性P-glycoprotein(P-gp) 抑制剂,Kd为 5.1 nM。
生物活性

Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor ofP-glycoprotein(P-gp) with the high affinity (Kd=5.1 nM)[1].

IC50& Target

Kd: 5.1 nM (P-gp)[1]

体外研究
(In Vitro)

Tariquidar (XR9576) is a potent modulator of P-gp mediated [3H]-Vinblastine and [3H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CHrB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC50=487±50 nM). [3H]-Tariquidar binds to CHrB30 membranes with the highest affinity (Kd=5.1±0.9 nM, n=7) and a binding capacity (Bmax) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of [3H]-Vinblastine is increased in a dose-dependent fashion by the modulators Tariquidar (EC50=487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC50value of 43±9 nM[1]. Tariquidar (XR9576) potentiates the cytotoxicity of several drugs including Doxorubicin, Paclitaxel, Etoposide, and Vincristine; complete reversal of resistance is achieved in the presence of 25-80 nM XR9576. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by [3H]Azidopine implying a direct interaction with the protein[2].

体内研究
(In Vivo)

In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar (XR9576) potentiates the antitumor activity of Doxorubicin without a significant increase in toxicity; maximum potentiation is observed at 2.5-4.0 mg/kg dosed either i.v. or p.o. In addition, coadministration of Tariquidar (6-12 mg/kg p.o.) fully restores the antitumor activity of Paclitaxel, Etoposide, and Vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. Tariquidar is found to also significantly potentiate the antitumor activity of doxorubicin against s.c. MC26 tumors in vivo[2].

Clinical Trial
分子量

719.65

Formula

C38H40Cl2N4O6

CAS 号

1992047-62-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.