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中文名称: Tariquidar methanesulfonate hydrate
英文名称: Tariquidar methanesulfonate hydrate
CAS No: 625375-83-9
分子式: C40H52N4O15S2
分子量: 893
安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)
T11027 Tariquidar methanesulfonate hydrate ≥98% (psaitong)
包装规格：
20mg in glass bottle
溶解性：
溶于DMSO(≥296mg/ml）
产品描述：

基本信息

产品编号：

T11027

产品名称：

Tariquidar methanesulfonate hydrate

CAS:

625375-83-9

 

储存条件

粉末

-20℃

四年

 

 

分子式：

C40H52N4O15S2

溶于液体

-80℃

6个月

分子量：

893.00

-20℃

1个月

化学名： 

N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide;methanesulfonic acid;trihydrate

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

1.1198mL

5.5992mL

11.1983mL

5mM

0.2240mL

1.1198mL

2.2397mL

10mM

0.1120mL

0.5599mL

1.1198mL

 

生物活性

产品描述

一种有效和特异性的P-glycoprotein(P-gp)抑制剂，Kd值为5.1nM。

靶点

Kd:5.1nM (P-gp)

 

体外研究

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 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 XR9576 (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 Tariquidar.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 methanesulfonate,hydrate (XR9576 methanesulfonate,hydrate) potentiates the antitumor activity of Doxorubicin without a significant increase in toxicity;maximum potentiation is observed at 2.5-4.0mg/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 ~4h,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 methanesulfonate 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) 1h 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.

Rat

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 methanesulfonate (10mg/kg).Tariquidar methanesulfonate 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℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
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