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  3. Dofequidar sesquifumarate

Dofequidar sesquifumarate  (Synonyms: MS-209 sesquifumarate)

目录号: HY-17013D
产品使用指南 技术支持

Dofequidar (MS-209) sesquifumarate 是一种具有口服活性喹啉化合物,可阻断 P-糖蛋白 (P-gp) 和多药耐药相关蛋白-1 (MDR-1)。Dofequidar sesquifumarate 对多药耐药肿瘤细胞具有很强的逆转作用。Dofequidar sesquifumarate 竞争性抑制 ABCB1/P-gp、ABCC1/MRP-1,阻断化疗剂的流出,增加癌细胞中的化疗剂浓度,增强化疗效果。

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Dofequidar sesquifumarate Chemical Structure

Dofequidar sesquifumarate Chemical Structure

CAS No. : 158681-49-3

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Dofequidar sesquifumarate 的其他形式现货产品:

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Other Forms of Dofequidar sesquifumarate:

Cell Viability Assay

    Dofequidar sesquifumarate purchased from MCE. Usage Cited in: Am J Transl Res. 2020 May 15;12(5):1807-1823.  [Abstract]

    CCK-8 assay showing a significantly lower cisplatin IC50 for the P-gp inhibitor Dofequidar fumarate (5 μM) treatment group compared with the vehicle control group in MG-63 and MNNG/HOS cells.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect[1][2].

    体外研究
    (In Vitro)

    Dofequidar sesquifumarate 在人小细胞肺癌 SBC-3/ADM 和 SBC-3 细胞体外增殖和药敏实验中,3-10 μM 可完全逆转 SBC-3/ADM 细胞对 Etoposide (VP-16) (HY-13629)、Adriamycin 和 Vincristine (HY-N0488) 的多药耐药性,对 SBC-3 细胞敏感性影响较小[1]
    Dofequidar sesquifumarate 在人小细胞肺癌 SBC-3/ADM 和 SBC-3 细胞 P-gp 表达分析实验中,未改变 SBC-3 细胞 P-gp 表达,SBC-3/ADM 细胞本身表达 P-gp[1]
    Dofequidar sesquifumarate 在多种癌细胞系的 SP 细胞分选实验中,以剂量依赖性方式降低侧群 (SP) 细胞的比例[2]
    Dofequidar sesquifumarate 在细胞内药物积累实验中增加 K562/BCRP 细胞中 ABCC1⁄MDR相关蛋白 (MRP) 的细胞内浓度[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Dofequidar(200 mg/kg;口服;从接种肿瘤细胞后第 10 或 14 天开始,共 4 次给药)sesquifumarate 在 NK 细胞耗竭的 SCID 小鼠(接种 SBC-3/ADM 或 SBC-3 细胞)模型中,与 Etoposide (VP-16) (HY-13629) 或 Adriamycin 联合使用显著抑制 SBC-3/ADM 细胞向多个器官的转移[1]
    Dofequidar(200 mg/kg;口服;在 Irinotecan (CPT-11) (HY-16562) 注射前 30 分钟给药,与 Irinotecan 一同在第 0、4、8 天给药)sesquifumarate 在接种 HeLa SP 细胞的裸鼠模型中,与 Irinotecan 联合使用显著减小肿瘤体积[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: 6- to 8-week-old male severe combined immunodeficiency (SCID) mice, depleted of natural killer (NK) cells by intraperitoneal injection of TM-β1 Ab (1 mg/mouse) 2 days before tumor inoculation, and then inoculated intravenously with SBC-3 or SBC-3/ADM cells[1]
    Dosage: 200 mg/kg
    Administration: Orally administered; the mice inoculated with SBC-3 cells were treated on days 14, 15, 21, and 22; the mice inoculated with SBC-3/ADM cells were treated on days 10, 11, 17, and 18.
    Result: Combined use with Etoposide (VP-16) (HY-13629) or Adriamycin can significantly inhibit metastasis formation by SBC-3/ADM cells to the liver, kidneys, and lymph nodes, and the weight of the liver of the treated mice was significantly less than that of other groups.
    Animal Model: 5- to 6-week-old female BALB/c-nu/nu (nude) mice, inoculated subcutaneously with HeLa SP cells[2]
    Dosage: 200 mg/kg
    Administration: Orally administered 30 minutes before intravenous injection of Irinotecan (67 mg/kg); on days 0, 4, and 8.
    Result: Co-treatment with Irinotecan drastically decreased the tumor volume.
    分子量

    1311.39

    Formula

    C30H31N3O3.3/2C4H4O4

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    纯度 & 产品资料
    参考文献
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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