| Identification | Back Directory | [Name]
dofequidar | [CAS]
129716-58-1 | [Synonyms]
dofequidar
Unii-0bjk6B565b
Dofequidar [inn]
4-(Diphenylacetyl)-alpha-[(5-quinolinyloxy)methyl]-1-piperazineethanol
1-(Diphenylacetyl)-4-((2rs)-2-hydroxy-3-(5-quinolyloxy)propyl)piperazine
1-[4-[2-Hydroxy-3-(5-quinolinyloxy)propyl]-1-piperazinyl]-2,2-diphenylethanone
Ethanone, 1-[4-[2-hydroxy-3-(5-quinolinyloxy)propyl]-1-piperazinyl]-2,2-diphenyl- | [Molecular Formula]
C30H31N3O3 | [MOL File]
129716-58-1.mol | [Molecular Weight]
481.59 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. |
| [storage]
Store at -20°C | [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 |
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SPIRO PHARMA
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Musechem
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DC Chemicals
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