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Dofequidar fumarate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Dofequidar fumarate图片
CAS NO:153653-30-6
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
据报道，Dofequidar fumarate (MS-209 fumarate) 是一种具有口服活性的喹啉化合物，可通过抑制 ABCB1/P-gp、ABCC1/MDR 相关蛋白 1 或两者来克服 MDR。
Cas No.153653-30-6
别名MS-209
化学名1-(4-(2-hydroxy-3-(quinolin-5-yloxy)propyl)piperazin-1-yl)-2,2-diphenylethanone fumarate
Canonical SMILESOC(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
分子式C34H35N3O7
分子量597.66
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.