Adjudin (Synonyms: AF-2364)
目录号: PL04855 纯度: ≥98%
CAS No. :252025-52-8
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中文名称
Adjudin
中文别名
1-(2,4-二氯苄基)-1H-吲唑-3-碳酰肼;男用口服避孕药
英文名称
Adjudin
英文别名
1-(2,4-Dichlorobenzyl)-1H-indazole-3-carbohydrazide;AF-2364;Adjudin;1-[(2,4-Dichlorophenyl)methyl]-1H-indazole-3-carboxylic acid hydrazide;AF 2364
Cas No.
252025-52-8
分子式
C15H12N4OCl2
分子量
335.19
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Adjudin 是一种广泛研究的男性避孕试剂,具有优越的线粒体抑制作用。 Adjudin 也是一种有效的 Cl- 通道阻断剂。
生物活性
Adjudin is an extensively studied male contraceptive with a superior mitochondria-inhibitory effect. Adjudin is also a potent Cl channel blocker.
性状
Solid
IC50 & Target[1][2]
Cl channel
Mitochondria
体外研究(In Vitro)
Adjudin is a potent blocker of Cl channels: disrupting Cl ion transport function results in a decline in sperm capacitation and fertilizing ability in humans in vitro. Adjudin (ADD) is a mitochondria inhibitor. Adjudin is a molecule that mediates adherens junction disruption at the Sertoli-germ cell interface. To investigate the effect of Adjudin on cancer cells, more than ten different types of human or mice cancer cell lines are treated with increasing concentrations of Adjudin and the cell proliferation is measured by the modified MTT assay. Adjudin inhibits cell proliferation in a dose dependent manner in SGC-7901 (human gastric adenocarcinoma cell), MDA-MB-231 (human breast adenocarcinoma cell), Smmc-7721 (human hepatoma cell) and MIA Paca-2 (human pancreatic adenocarcinoma cell) cells. The IC50 of Adjudin is determined to be 58.0 μM, 13.8 μM, 72.3 μM and 52.7
体内研究(In Vivo)
To determine whether Adjudin can inhibit lung and prostate cancer growth in vivo, the effect of Adjudin is tested in a subcutaneous model of lung and prostate cancer. Human lung carcinoma cells A549 and prostate carcinoma cells PC3 are injected into athymic nude mice subdermally at the lower back site respectively. Mice are then randomized into two treatment groups with similar mean tumor sizes: Adjudin and vehicle (control). Approximately 2 weeks after tumor inoculation Adjudin is injected intraperitoneally once every three days in lung carcinoma cells and every other day in prostate carcinoma cells at 100 mg/kg. Adjudin treatment can be well tolerated in rodent. And Adjudin-treated mice show significant tumor growth inhibition compared with the control group (P<0.0001 in the human lung carcinoma cells A549 and P=0.006 in the prostate carcinoma cells PC3).
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Li K, et al. Inhibition of sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans. Hum Reprod. 2013 Jan;28(1):47-59.
[2]. Li X, et al. Combination delivery of Adjudin and Doxorubicin via integrating drug conjugation and nanocarrier approaches for the treatment of drug-resistant cancer cells. J Mater Chem B. 2015 Feb 28;3(8):1556-1564.
溶解度数据
In Vitro: DMSO : 16.67 mg/mL (49.73 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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