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1992047-62-7

英文名稱 Tariquidar dihydrochloride
CAS 1992047-62-7
分子式 C38H39ClN4O6
分子量 683.2
MOL 文件 1992047-62-7.mol
更新日期 2025/01/12 18:03:36
1992047-62-7 結構式 1992047-62-7 結構式

基本信息

英文別名
Tariquidar dihydrochloride

物理化學性質

儲存條件-20°C儲存
溶解度溶于二甲基亞砜

常見問題列表

生物活性
Tariquidar dihydrochloride (XR9576 dihydrochloride) 是一種有效的特異性 P-glycoprotein (P-gp) 抑制劑,Kd 為 5.1 nM。
靶點

Kd: 5.1 nM (P-gp)

體外研究

Tariquidar (XR9576) is a potent modulator of P-gp mediated [ 3 H]-Vinblastine and [ 3 H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CH r B30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC 50 =487±50 nM). [ 3 H]-Tariquidar binds to CH r B30 membranes with the highest affinity (K d =5.1±0.9 nM, n=7) and a binding capacity (B max ) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of [ 3 H]-Vinblastine is increased in a dose-dependent fashion by the modulators Tariquidar (EC 50 =487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC 50 value of 43±9 nM. 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 [ 3 H]Azidopine implying a direct interaction with the protein.

體內研究

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.

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