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dofequidar

dofequidar Structure
dofequidar
  • CAS No.129716-58-1
  • Chemical Name:dofequidar
  • CBNumber:CB01856039
  • Molecular Formula:C30H31N3O3
  • Formula Weight:481.59
  • MOL File:129716-58-1.mol
dofequidar Property
  • Boiling point 720.8±60.0 °C(Predicted)
  • Density 1.228
  • storage temp. Inert atmosphere,Store in freezer, under -20°C
  • solubility Soluble in DMSO
  • form Powder
  • pka 13.94±0.20(Predicted)
  • color White to off-white
  • FDA UNII 0BJK6B565B
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements
  • Precautionary statements

dofequidar Chemical Properties,Usage,Production

  • Uses Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar 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].
  • in vivo

    Dofequidar (200 mg/kg; orally administered; starting from days 10 or 14 after tumor cell inoculation, 4 doses) 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) in nude mice inoculated with HeLa SP cells significantly reduces the tumor volume when combined with Irinotecan[2].

    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.
  • References [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. DOI:10.1111/j.1349-7006.2001.tb01162.x
    [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. DOI:10.1111/j.1349-7006.2009.01288.x
dofequidar Preparation Products And Raw materials
Raw materials
Preparation Products
dofequidar Suppliers
Global(36)Suppliers
  • Supplier：
    LEAPCHEM CO., LTD.
  • Tel：+86-852-30606658
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  • Supplier： LETOPHARM LIMITED
  • Tel：+86-21-5821 5861
  • Email：sales@letopharm.com
  • Country：China
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  • Supplier： SPIRO PHARMA
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  • Email：eric_feng1954@126.com
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dofequidar Spectrum
129716-58-1, dofequidarRelated Search:
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  • Unii-0bjk6B565b
  • Dofequidar [inn]
  • 1-(Diphenylacetyl)-4-((2rs)-2-hydroxy-3-(5-quinolyloxy)propyl)piperazine
  • dofequidar

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