Tariquidar methanesulfonate, hydrate
- Tariquidar methanesulfonate hydrate,XR 9576,XR-9576
货号: abs811447
货号-规格 | 货期 | 价格 | 数量 |
abs811447-10mg | 4周 | ¥950.00 | - + |
abs811447-50mg | 4周 | ¥2950.00 | - + |

产品描述 | ||
描述 | XR9576 is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer | |
纯度 | >98% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
别名 | Tariquidar methanesulfonate hydrate,XR 9576,XR-9576 | |
可溶性/溶解性 | DMSO: ≥ 296 mg/mL; H2O: < 8.9 mg/mL | |
生物活性 | ||
靶点 | P-glycoprotein | |
In vitro(体外研究) | Tariquidar (XR9576) methanesulfonate is a potent modulator of P-gp mediated -Vinblastine and -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). -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 -Vinblastine is increased in a dose-dependent fashion by the modulators XR9576 (EC50=487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC50 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 Tariquidar. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by Azidopine implying a direct interaction with the protein. | |
In vivo(体内研究) | In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar (XR9576) methanesulfonate 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. | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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