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Tariquidar methanesulfonate, hydrate

CAS No. : 625375-83-9

MCE 站：Tariquidar methanesulfonate, hydrate

产品活性：Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) 是有效和特异性的 P-glycoprotein (P-gp) 抑制剂，K_d值为5.1 nM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P-glycoprotein

In Vitro: Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) 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 CH^rB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC₅₀=487±50 nM). [³H]-Tariquidar binds to CH^rB30 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 [³H]-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 [³H]Azidopine implying a direct interaction with the protein.

In Vivo: In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) 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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