Dofequidar fumarate (Synonyms: MS-209) |
| カタログ番号GC13375 |
経口活性キノリン化合物であるフマル酸ドフェキダル (MS-209 フマル酸) は、ABCB1/P-gp、ABCC1/MDR 関連タンパク質 1、またはその両方を阻害することによって MDR を克服することが報告されています。
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Cas No.: 153653-30-6
Sample solution is provided at 25 µL, 10mM.
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Dofequidar fumarate is a multidrug-resistant (MDR) - reversal agent [1].
Dofequidar fumarate is a quinoline derivative and has highly potent reversing effect on multidrug-resistant tumor cells. It prevents the transport of antitumor drugs through interacting with the drug-efflux pump P-glycoprotein directly and thereby reverses MDR. In vincristine (VCR)-resistant P388/VCR cells and Adriamycin (ADM)- resistant P388/ADM cells, dofequidar fumarate at 1μM and 3μM can completely reverse the drug resistance. It also shows significant effects on the MDR K562 cells. Furthermore, in mice model bearing HCT-15 xenografts, combination therapy of dofequidar fumarate and docetaxel induces remarkable tumor growth inhibition. Dofequidar fumarate also shows significant reversing effect in MCF-7/ADM-bearing mice [1, 2].
References:
[1] Sato W, Fukazawa N, Nakanishi O, et al. Reversal of multidrug resistance by a novel quinoline derivative, MS-209. Cancer chemotherapy and pharmacology, 1995, 35(4): 271-277.
[2] Naito M, Matsuba Y, Sato S, et al. MS-209, a quinoline-type reversal agent, potentiates antitumor efficacy of docetaxel in multidrug-resistant solid tumor xenograft models. Clinical cancer research, 2002, 8(2): 582-588.
| Cas No. | 153653-30-6 | SDF | |
| 同義語 | MS-209 | ||
| Chemical Name | 1-(4-(2-hydroxy-3-(quinolin-5-yloxy)propyl)piperazin-1-yl)-2,2-diphenylethanone fumarate | ||
| Canonical SMILES | OC(COC1=CC=CC2=C1C=CC=N2)CN3CCN(C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)CC3.O=C(O)/C([H])=C([H])/C(O)=O | ||
| Formula | C34H35N3O7 | M.Wt | 597.66 |
| 溶解度 | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6732 mL | 8.366 mL | 16.7319 mL |
| 5 mM | 0.3346 mL | 1.6732 mL | 3.3464 mL |
| 10 mM | 0.1673 mL | 0.8366 mL | 1.6732 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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