Dofequidar fumarate
Based on 2 publication(s) in Google Scholar
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.
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- Reinheit: 98.0%
- CAS. Nr.: 153653-30-6
- Formel: C34H35N3O7
- Molecular Weight:597.66
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Dofequidar fumarate
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Cell Proliferation/Viability Assay
Biologische Aktivität
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:200 mg/kg
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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.
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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.
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Animal Model:5- to 6-week-old female BALB/c-nu/nu (nude) mice, inoculated subcutaneously with HeLa SP cells[2]
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Dosage:200 mg/kg
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Administration:Orally administered 30 minutes before intravenous injection of Irinotecan (67 mg/kg); on days 0, 4, and 8.
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Result:Co-treatment with Irinotecan drastically decreased the tumor volume.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 153653-30-6
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Appearance Solid
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Molecular Weight 597.66
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Formel C34H35N3O7
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Color White to off-white
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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
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Synonyms
MS-209
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Am J Transl Res
MARK2 enhances cisplatin resistance via PI3K/AKT/NF-κB signaling pathway in osteosarcoma cells. [Abstract]2020 May 15;12(5):1807-1823. PMID: 32509178
Dofequidar fumarate purchased from MedChemExpress. Usage Cited in: Am J Transl Res. 2020 May 15;12(5):1807-1823. [Abstract]
CCK-8 assay showing a significantly lower cisplatin IC50 for the P-gp inhibitor Dofequidar fumarate (5 μM) treatment group compared with the vehicle control group in MG-63 and MNNG/HOS cells.
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Anticancer Res
P-Glycoprotein Overexpression Is Associated With Cisplatin Resistance in Human Osteosarcoma. [Abstract]2019 Apr;39(4):1711-1718. PMID: 30952710
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (167.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (1.67 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.6732 mL | 8.3660 mL | 16.7319 mL | 41.8298 mL |
| DMSO | 5 mM | 0.3346 mL | 1.6732 mL | 3.3464 mL | 8.3660 mL |
| 10 mM | 0.1673 mL | 0.8366 mL | 1.6732 mL | 4.1830 mL | |
| 15 mM | 0.1115 mL | 0.5577 mL | 1.1155 mL | 2.7887 mL | |
| 20 mM | 0.0837 mL | 0.4183 mL | 0.8366 mL | 2.0915 mL | |
| 25 mM | 0.0669 mL | 0.3346 mL | 0.6693 mL | 1.6732 mL | |
| 30 mM | 0.0558 mL | 0.2789 mL | 0.5577 mL | 1.3943 mL | |
| 40 mM | 0.0418 mL | 0.2091 mL | 0.4183 mL | 1.0457 mL | |
| 50 mM | 0.0335 mL | 0.1673 mL | 0.3346 mL | 0.8366 mL | |
| 60 mM | 0.0279 mL | 0.1394 mL | 0.2789 mL | 0.6972 mL | |
| 80 mM | 0.0209 mL | 0.1046 mL | 0.2091 mL | 0.5229 mL | |
| 100 mM | 0.0167 mL | 0.0837 mL | 0.1673 mL | 0.4183 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Dofequidar fumarate Related Classifications
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