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Dofequidar fumarate

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产品编号 T11071Cas号 153653-30-6
别名 MS-209

Dofequidar fumarate (MS-209) 是口服活性的喹啉化合物,通过抑制 ABCB1/P-gp 和 ABCC1/MDR 相关蛋白 1 来克服 MDR。

Dofequidar fumarate

Dofequidar fumarate

Rating icon 很棒
纯度: 99.43%
产品编号 T11071 别名 MS-209Cas号 153653-30-6

Dofequidar fumarate (MS-209) 是口服活性的喹啉化合物,通过抑制 ABCB1/P-gp 和 ABCC1/MDR 相关蛋白 1 来克服 MDR。

规格价格库存数量
1 mg
¥ 339
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2 mg
¥ 492
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5 mg
¥ 813
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10 mg
¥ 1,290
现货
25 mg
¥ 2,360
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50 mg
¥ 3,520
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100 mg
¥ 4,970
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500 mg
¥ 10,700
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1 mL x 10 mM (in DMSO)
¥ 995
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产品介绍

生物活性
产品描述
Dofequidar fumarate (MS-209)(MS-209 fumarate), a quinoline-based compound administered orally, is known for counteracting multidrug resistance (MDR) through the inhibition of ABCB1/P-glycoprotein (P-gp) and ABCC1/MDR-associated protein 1.
体外活性
Dofequidar fumarate effectively overcomes docetaxel resistance in MDR cancer cells, and this concentration reaches> 7 h in plasma without severe toxicity.Dofequidar fumarate restored the chemical sensitivity of SBC-3/ADM cells to VP-16, ADM and VCR in a dose-dependent manner in vitro. Dofequidar inhibits the outflow of chemotherapy drugs and increases the sensitivity of anti-cancer drugs to CSC-like side population (SP) cells isolated from various cancer cell lines. Dofequidar treatment greatly reduces the number of cells in the SP component. In 4-1St cells with strong resistance to ADM and VCR, Dofequidar fumarate at a concentration of 3 microM increased the cytotoxicity of ADM and VCR by 88-fold and 350-fold, respectively.
体内活性
Docetaxel alone at the maximum tolerated dose (MTD) has significant antitumor activity against intrinsically resistant HCT-15 tumor xenografts, while Dofequidar fumarate also enhances the antitumor effect of docetaxel active. For MCF-7/ADM tumor xenografts expressing large amounts of P-gp, docetaxel alone did not show antitumor activity at MTD, while the combination of MTD and Dofequidar fumarate for docetaxel greatly reduced MCF -7/ADM tumor growth. Intravenous injection of SBC-3 or SBC-3/ADM cells will produce metastatic colonies in the liver, kidneys, and lymph nodes in severe combined immunodeficiency (SCID) mice depleted by natural killer (NK) cells, although SBC-3/ ADM cells produce faster transfers than SBC-3 cells. The treatment of VP-16 and ADM reduced the formation of metastasis of SBC-3 cells, while the same treatment did not affect the metastasis of SBC-3/ADM cells. Although the use of MS-209 alone has no effect on the transfer of SBC-3 or SBC-3/ADM cells, the combined use of MS-209 and VP-16 or ADM can significantly inhibit the proliferation of SBC-3/ADM cells Metastasis to form an organ.
别名MS-209
化学信息
分子量597.66
分子式C34H35N3O7
CAS No.153653-30-6
SmilesOC(=O)\C=C\C(O)=O.OC(COc1cccc2ncccc12)CN1CCN(CC1)C(=O)C(c1ccccc1)c1ccccc1
密度no data available
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: 1 mg/mL (1.67 mM), Sonication is recommended.
DMSO: 100 mg/mL (167.32 mM), Sonication is recommended.
溶液配制表
H2O/DMSO
1mg5mg10mg50mg
1 mM1.6732 mL8.3660 mL16.7319 mL83.6596 mL
DMSO
1mg5mg10mg50mg
5 mM0.3346 mL1.6732 mL3.3464 mL16.7319 mL
10 mM0.1673 mL0.8366 mL1.6732 mL8.3660 mL
20 mM0.0837 mL0.4183 mL0.8366 mL4.1830 mL
50 mM0.0335 mL0.1673 mL0.3346 mL1.6732 mL
100 mM0.0167 mL0.0837 mL0.1673 mL0.8366 mL

SCI 文献

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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