Dofequidar fumarate
(Synonyms: MS-209) 目录号 : GC13375
A quinoline derivative and inhibitor of multidrug resistance
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 | |
| 别名 | MS-209 | ||
| 化学名 | 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 | ||
| 分子式 | C34H35N3O7 | 分子量 | 597.66 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet