dofequidar
dofequidar Basic information
- Product Name:
- dofequidar
- Synonyms:
-
- dofequidar
- 1-(Diphenylacetyl)-4-((2rs)-2-hydroxy-3-(5-quinolyloxy)propyl)piperazine
- Dofequidar [inn]
- Unii-0bjk6B565b
- 1-[4-[2-Hydroxy-3-(5-quinolinyloxy)propyl]-1-piperazinyl]-2,2-diphenylethanone
- 4-(Diphenylacetyl)-alpha-[(5-quinolinyloxy)methyl]-1-piperazineethanol
- Ethanone, 1-[4-[2-hydroxy-3-(5-quinolinyloxy)propyl]-1-piperazinyl]-2,2-diphenyl-
- 1-(4-(2-Hydroxy-3-(quinolin-5-yloxy)propyl)piperazin-1-yl)-2,2-diphenylethan-1-one
- CAS:
- 129716-58-1
- MF:
- C30H31N3O3
- MW:
- 481.59
- Mol File:
- 129716-58-1.mol
dofequidar Chemical Properties
- 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
dofequidar Usage And Synthesis
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. |
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
dofequidarSupplier
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- +86-21-5821 5861
- sales@letopharm.com
- Tel
- eric_feng1954@126.com
- Tel
- 021-65675885 18964387627
- info@efebio.com
- Tel
- 0-2022843681 15618226720
- chaolaichem@foxmail.com