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• 产品描述： Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1

• 靶点： P-gp

• 体外研究：
  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.

• 体内研究：
  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.

• 参考文献：
  1. Katayama R, et al. Dofequidar fumarate sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export. Cancer Sci. 2009 Nov;100(11):2060-8. 2. Nokihara H, et al. A new quinoline derivative MS-209 reverses multidrug resistance and inhibits multiorgan metastases by P-glycoprotein-expressing human small cell lung cancer cells. Jpn J Cancer Res. 2001 Jul;92(7):785-92. 3. Nakanishi O, et al. Potentiation of the antitumor activity by a novel quinoline compound, MS-209, in multidrug-resistant solid tumor cell lines. Oncol Res. 1997;9(2):61-9. 4. Naito M, et al. MS-209, a quinoline-type reversal agent, potentiates antitumor efficacy of docetaxel in multidrug-resistant solid tumor xenograft models. Clin Cancer Res. 2002 Feb;8(2):582-8.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.673 ml	8.366 ml	16.732 ml
  5 mM	0.335 ml	1.673 ml	3.346 ml
  10 mM	0.167 ml	0.837 ml	1.673 ml
  50 mM	0.033 ml	0.167 ml	0.335 ml

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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 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *