Dofequidar sesquifumarate  (Synonyms: MS-209 sesquifumarate)

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].

Dofequidar sesquifumarate in the in vitro proliferation and chemosensitivity assays of human small cell lung cancer SBC-3/ADM and SBC-3 cells completely reverses the multidrug resistance of SBC-3/ADM cells to Etoposide (VP-16) (HY-13629), Adriamycin, and Vincristine (HY-N0488) at concentrations of 3-10 μM, with little effect on the sensitivity of SBC-3 cells^[1].
Dofequidar sesquifumarate in the P-gp expression analysis experiment of human small cell lung cancer SBC-3/ADM and SBC-3 cells does not change the P-gp expression of SBC-3 cells, while SBC-3/ADM cells express P-gp^[1].
Dofequidar sesquifumarate at various concentrations reduces the proportion of side population (SP) cells in a dose-dependent manner in the SP cell sorting experiment of multiple cancer cell lines^[2].
Dofequidar sesquifumarate increases the intracellular concentration of ABCC1⁄MDR-associated protein (MRP) in K562/BCRP cells in the intracellular drug accumulation experiment^[2].

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

Dofequidar (200 mg/kg; orally administered; starting from days 10 or 14 after tumor cell inoculation, 4 doses) sesquifumarate in NK cell-depleted SCID mice inoculated with SBC-3/ADM or SBC-3 cells significantly inhibits the metastasis of SBC-3/ADM cells to multiple organs when combined with Etoposide (VP-16) (HY-13629) or Adriamycin^[1].
Dofequidar (200 mg/kg; orally administered; given 30 minutes before Irinotecan (CPT-11) (HY-16562) injection, and both are administered on days 0, 4, and 8; throughout the experiment) sesquifumarate in nude mice inoculated with HeLa SP cells significantly reduces the tumor volume when combined with Irinotecan^[2].

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

1311.39

C₃₀H₃₁N₃O₃.3/2C₄H₄O₄

158681-49-3

OC(COC1=C2C=CC=NC2=CC=C1)CN3CCN(C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)CC3.O=C(O)/C=C/C(O)=O.[1.5]

Room temperature in continental US; may vary elsewhere.

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

• [1]. 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.  [Content Brief]

  [2]. 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.  [Content Brief]