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Tariquidar methanesulfonate, hydrate is a potent and specific P-glycoprotein (P-gp) inhibitor(Kd of 5.1 nM).
Tariquidar methanesulfonate, hydrate is a potent and specific P-glycoprotein (P-gp) inhibitor(Kd of 5.1 nM).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 mg | ¥ 10,900 | 期货 |
产品描述 | Tariquidar methanesulfonate, hydrate is a potent and specific P-glycoprotein (P-gp) inhibitor(Kd of 5.1 nM). |
靶点活性 | P-gp:(kd)5.1 nM |
体外活性 | Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent P-gp mediated [3H]-Vinblastine modulator 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 with EC50 of 487±50 nM. [3H]-Tariquidar binds to CHrB30 membranes with the highest affinity with Kd of 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 XR9576 with EC50 of 487±50 nM. The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity(IC50 of 43±9 nM)[1]. Tariquidar 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[2]. |
体内活性 | In mice with intrinsically resistant MC26 colon tumors, co-administration of hydrated Tariquidar mesylate (XR9576 mesylate, hydrate) can enhance the antitumor activity of doxorubicin without significantly increasing 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]. |
别名 | XR9576 methanesulfonate, hydrate |
分子量 | 892.99 |
分子式 | C40H52N4O15S2 |
CAS No. | 625375-83-9 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 296 mg/mL (331.47 mM) H2O: 5 mg/mL (5.60 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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