Dofequidar

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Chemical Structure| 129716-58-1 同义名 : -
CAS号 : 129716-58-1
货号 : A178453
分子式 : C30H31N3O3
纯度 : 98%
分子量 : 481.59
MDL号 : N/A
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Dofequidar(MS-209) is a novel quinoline compound, which can reverse P-glycoprotein (P-gp)-mediated MDR. In cell-based studies, MS-209 at 3 μM successfully mitigated docetaxel resistance in MDR cancer cells, maintaining this concentration in blood plasma for over 7 hours without significant toxicity[1]. MS-209 reinstates the sensitivity of SBC-3 / ADM cells to VP-16, ADM, and VCR in a dose-dependent manner[2]. MS-209 significantly reverses resistance to adriamycin (ADM) and vincristine (VCR) in established MDR tumor cell lines, such as 2780AD and KB-C1, and enhances the cytotoxic effects of ADM and VCR on a variety of human and mouse cell lines. Notably, in 4-1St cells, which show high resistance to ADM and VCR, a 3 μM concentration of MS-209 boosts the cytotoxicity of ADM and VCR by 88 and 350 times, respectively. Administering docetaxel at its maximal tolerated dose (MTD) demonstrated noticeable antitumor effects on HCT-15 tumor xenografts, known for their intrinsic resistance, with MS-209 further enhancing docetaxel's antitumor efficacy. In the case of MCF-7/ADM tumor xenografts, which express higher levels of P-gp, docetaxel alone at the MTD failed to exhibit antitumor effects. However, when combined with MS-209, the MTD of docetaxel significantly inhibited the growth of MCF-7/ADM tumors[1]. Intravenous injection of SBC-3 or SBC-3/ADM cells into severe combined immunodeficiency (SCID) mice, depleted of natural killer (NK) cells, resulted in metastatic colonies forming in the liver, kidneys, and lymph nodes, with SBC-3/ADM cells leading to quicker metastasis than SBC-3 cells. While VP-16 and ADM treatments reduced metastasis from SBC-3 cells, they did not affect metastasis from SBC-3/ADM cells. Although MS-209 alone did not impact metastasis from either cell type, its combination with VP-16 or ADM significantly reduced metastatic spread of SBC-3/ADM cells to various organs[2]. Oral administration of MS-209 along with ADM substantially increased the antitumor effects of ADM on Colon 26 and 4-1St tumors implanted subcutaneously in mice, surpassing the antitumor efficacy of ADM alone at its MTD[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.38mL

2.08mL

1.04mL

20.76mL

4.15mL

2.08mL
参考文献

[1]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.

[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.