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Tariquidar dihydrochloride  

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包装规格：100mg in glass bottle
产品描述：基本信息 产品编号： T11029 产品名称： Tariquidar dihydrochloride CAS: 1992047-62-7   储存条件 粉末 -20℃ 四年 分子式： C38H40Cl2N4O6 溶于液体 -80℃ 二年 分子量： 719.65     化学名：  N-[2-[[[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-3-quinolinecarbxamide dihydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 一种有效的特异性P-glycoprotein(P-gp)抑制剂，Kd为5.1nM。 靶点 Kd:5.1nM (P-gp)   体外研究 Tariquidar (XR9576) 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 CHrB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC50=487±50nM).[3H]-Tariquidar binds to CHrB30 membranes with the highest affinity (Kd=5.1±0.9nM,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 Tariquidar (EC50=487±50nM).The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity,with potent IC50 value of 43±9nM.Tariquidar (XR9576) potentiates the cytotoxicity of several drugs including Doxorubicin,Paclitaxel,Etoposide,and Vincristine;complete reversal of resistance is achieved in the presence of 25-80nM XR9576.Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by [3H]Azidopine implying a direct interaction with the protein. 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 2.5-4.0mg/kg dosed either i.v.or p.o. In addition,coadministration of Tariquidar (6-12mg/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.   推荐实验方法(仅供参考) 细胞实验:   Cells (EMT6 AR1.0 8×102/well;A2780 5×103/well;2780AD 6×103/well) are seeded into 96-well plates.After ~4 h, varying concentrations of Tariquidar are added, and cells are incubated for an additional 4 days (EMT6 AR1.0) or 6 days (2780AD) before quantification of cell growth and calculation of IC10 values (concentration resulting in 10% inhibition of cell growth).   动物实验:   Mice MC26 tumor slurry is implanted s.c.in BALB/c mice (day 0).The animals are then randomized,24h later,into groups of 15-18 and treated once with various regimens.Tariquidar or vehicle is administered either i.v.via a lateral tail vein or p.o.with Doxorubicin (5mg/kg) or vehicle i.v.The modulator is administered either i.v.at 2-4mg/kg (10mL/kg) at the same time as Doxorubicin or p.o.at 2-8mg/kg (10mL/kg) 1 h before the Cytotoxic drug.GG918 is administered p.o.1h before doxorubicin.All of the animals are weighed twice weekly.The animals are killed by cervical dislocation on day 14,and the tumors are excised and weighed. The data are analyzed by Student’s t test. Rats Male CD rats (3 animals per time point) are dosed i.v.with paclitaxel alone [15 min infusion at 10mg/kg in Tween 80:ethanol:5% dextrose (5:10:85% v/v/v)] or in combination with Tariquidar (10mg/kg).Tariquidar is administered as a bolus (i.v.) dose 15 min before infusion of Paclitaxel.Blood samples are collected by cardiac puncture using heparinized syringes at various times between 0.083 and 48h and are centrifuged to prepare plasma,which is stored at −20℃ until analysis.Paclitaxel concentration in plasma samples is measured by a LC-MS/MS assay.
保存条件：-20℃

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