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MS 209

MS 209 Structure
MS 209
  • CAS No.158681-49-3
  • Chemical Name:MS 209
  • CBNumber:CB81390656
  • Molecular Formula:C30H31N3O3.C4H4O4
  • Formula Weight:597.664
  • MOL File:158681-49-3.mol
MS 209 Property
  • storage temp. -20°C
  • solubility DMSO: soluble20mg/mL, clear
  • form powder
  • color white to beige
  • NCI Dictionary of Cancer Terms MS 209
  • FDA UNII 3DM793MFSE
Safety
  • WGK Germany  :3
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H361-H412
  • Precautionary statements P264-P270-P301+P312-P330-P501-P201-P202-P281-P308+P313-P405-P501-P273-P501

MS 209 Chemical Properties,Usage,Production

  • Uses 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].
  • in vivo

    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].

    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
MS 209 Preparation Products And Raw materials
Raw materials
Preparation Products
MS 209 Suppliers
Global(13)Suppliers
  • Supplier: Energy Chemical
  • Tel:021-58432009<br/>400-005-6266
  • Email:marketing@energy-chemical.com
  • Country:China
  • ProdList:44918
  • Advantage:58
MS 209 Spectrum
158681-49-3, MS 209Related Search:
  • 细胞生物学试剂
  • ABCB1/P-GP/ABCC1/MDR-相关蛋白1抑制剂(DOFEQUIDAR FUMARATE)
  • 158681-49-3
  • Dofequidar (sesquifumarate)
  • Dofequidar fumarate >=98% (HPLC)
  • MS-209 fumarate
  • 4-(Diphenylacetyl)-a-[(5-quinolinyloxy)methyl]-1-Piperazineethanol (E)-2-butenedioate fumarate (1:1.5)
  • Dofequidar fumarate
  • 4-(Diphenylacetyl)-alpha-((5-quinolinyloxy)methyl)-1-piperazineethanol (E)-2-butenedioate (2:3) (salt)
  • 1-Piperazineethanol, 4-(diphenylacetyl)-alpha-((5-quinolinyloxy)methyl)-, (E)-2-butenedioate (2:3) (salt)
  • MS 209