2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. 129716-58-1

129716-58-1

Dofequidar Chemical Structure

129716-58-1

Chemical Structure

  • Dofequidar
  • Synonym(s): MS-209 free base
  • CAS No: 129716-58-1
    Formula: C30H31N3O3
    Molecular Weight: 481.59
  • IUPAC Name: 1-(4-(2-hydroxy-3-(quinolin-5-yloxy)propyl)piperazin-1-yl)-2,2-diphenylethan-1-one
  • InChIKey: KLWUUPVJTLHYIM-UHFFFAOYSA-N
  • SMILES: OC(COC1=C2C=CC=NC2=CC=C1)CN3CCN(C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)CC3

Biological Activity: 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].

Cat. No. Product Name Purity Description
HY-17013 Dofequidar 98.17% 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.

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. [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]

Keywords:

Dofequidar