Dofequidar (fumarate)
CAS No. : 153653-30-6
(Synonyms: MS-209)
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|---|---|---|
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| 10mg | $156 | In-stock |
| 50mg | $600 | In-stock |
| 100mg | $1020 | In-stock |
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| Cat. No. : | HY-17013A |
| M.Wt: | 597.66 |
| Formula: | C34H35N3O7 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic);H2O : 1 mg/mL (ultrasonic) |
Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate 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 Vitro:Dofequidar fumarate 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 fumarate 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 fumarate 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 fumarate increases the intracellular concentration of ABCC1⁄MDR-associated protein (MRP) in K562/BCRP cells in the intracellular drug accumulation experiment[2].
In Vivo:Dofequidar (200 mg/kg; orally administered; starting from days 10 or 14 after tumor cell inoculation, 4 doses) fumarate 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) fumarate in nude mice inoculated with HeLa SP cells significantly reduces the tumor volume when combined with Irinotecan[2].
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