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抑制剂/激活剂

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凋亡与自噬

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Tariquidar XR9576

Tariquidar是一种有效的，选择性的，非竞争性P-glycoprotein抑制剂，在CHrB30细胞系中Kd为5.1 nM，作用于MDR细胞系逆转耐药性。Phase 3。

货号：
TK0222
规格：

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	206873-63-4
生物活性	Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
分子式	C38H38N4O6
分子量	646.73
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 25 mg/mL (38.66 mM; ultrasonic and adjust pH to 5 with HCl) H2O : < 0.1 mg/mL (insoluble)
体内研究	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.
体外研究	Tariquidar (XR9576) is a potent modulator of P-gp mediated [H]-Vinblastine and [H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CHB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC50=487±50 nM). [H]-Tariquidar binds to CHB30 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 [H]-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 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 XR9576. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by [H]Azidopine implying a direct interaction with the protein.
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纯度及产品资料	98%

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