Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 339 | 现货 | ||
2 mg | ¥ 492 | 现货 | ||
5 mg | ¥ 813 | 现货 | ||
10 mg | ¥ 1,290 | 现货 | ||
25 mg | ¥ 2,360 | 现货 | ||
50 mg | ¥ 3,520 | 现货 | ||
100 mg | ¥ 4,970 | 现货 | ||
500 mg | ¥ 10,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 995 | 现货 |
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 |
分子量 | 597.66 |
分子式 | C34H35N3O7 |
CAS No. | 153653-30-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 1 mg/mL (1.67 mM), Sonication is recommended.
DMSO: 100 mg/mL (167.32 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 1.6732 mL | 8.366 mL | 16.7319 mL | 41.8298 mL |
DMSO | 5 mM | 0.3346 mL | 1.6732 mL | 3.3464 mL | 8.366 mL |
10 mM | 0.1673 mL | 0.8366 mL | 1.6732 mL | 4.183 mL | |
20 mM | 0.0837 mL | 0.4183 mL | 0.8366 mL | 2.0915 mL | |
50 mM | 0.0335 mL | 0.1673 mL | 0.3346 mL | 0.8366 mL | |
100 mM | 0.0167 mL | 0.0837 mL | 0.1673 mL | 0.4183 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Dofequidar fumarate 153653-30-6 Membrane transporter/Ion channel Neuroscience P-gp Dofequidar Inhibitor CD243 ABCB1 Dofequidar Fumarate Multidrug resistance protein 1 Cluster of differentiation 243 MS-209 P-glycoprotein MDR1 inhibit MS 209 MS209 Pgp inhibitor