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Dofequidar (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].

Product Specifications

CAS Number

[158681-49-3]

Product Name Alternative

MS-209 (sesquifumarate)

UNSPSC

12352005

Hazard Statement

H302-H361-H412

Target

P-glycoprotein

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/dofequidar-sesquifumarate.html

Smiles

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]

Molecular Formula

C30H31N3O3.3/2C4H4O4

Molecular Weight

1311.39

Precautions

P264-P270-P273-P280-P330-P405-P501

References & Citations

[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.|[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 1

Curated Selection

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