CIS-TRIMETHOXY STILBENE(94608-23-8)

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CIS-TRIMETHOXY STILBENE 製品概要
化学名:
英語化学名:CIS-TRIMETHOXY STILBENE
别名:1,3-DIMETHOXY-5-[(1Z)-2-(4-METHOXYPHENYL)ETHENYL]-BENZENE;CIS-TRIMETHOXY STILBENE;CIS-TRISMETHOXY RESVERATROL;(Z)-3,5,4'-Trimethoxystilbene;1,2,3-trimethoxy-4-(2-phenylethenyl)benzene;1,3-dimethoxy-5-[(Z)-2-(4-methoxyphenyl)ethenyl]benzene;(Z)-1-(3,5-dimethoxyphenyl)-2-(4-methoxyphenyl)ethene;Benzene, 1,3-dimethoxy-5-[(1Z)-2-(4-methoxyphenyl)ethenyl]-
CAS番号:94608-23-8
分子式:C17H18O3
分子量:270.32
EINECS:
カテゴリ情報:
Mol File:94608-23-8.mol
CIS-TRIMETHOXY STILBENE
CIS-TRIMETHOXY STILBENE 物理性質
融点 55-57 °C
沸点 423.8±35.0 °C(Predicted)
比重(密度) 1.104±0.06 g/cm3(Predicted)
貯蔵温度 Store at -20°C
溶解性≤50mg/ml in DMSO;50mg/ml in dimethyl formamide
外見 solution in ethanol.
CAS データベース94608-23-8
安全性情報
主な危険性 Xi
Rフレーズ 41
Sフレーズ 26-39
MSDS Information
CIS-TRIMETHOXY STILBENE Usage And Synthesis
説明Resveratrol is a potent antioxidant found in grapes and red wine that also has anti-proliferative, anti-neoplastic and anti-angiogenic activities. In addition, resveratrol activates sirtuins and, in yeast, extends lifespan. cis-trismethoxy Resveratrol is a potent anti-mitotic drug that is 100-fold more active than resveratrol at inhibiting the growth of human colon cancer Caco-2 cells. It inhibits tubulin polymerization in a dose-dependent manner (IC50 = 4 μM) and inhibits enzymes involved in the synthesis of the polyamines, putrescine, and spermidine. trans-trismethoxy Resveratrol has superior pharmacokinetic characteristics when compared with resveratrol, including greater plasma exposure, longer elimination half-life, and lower clearance.
使用cis-trismethoxy Resveratrol is a potent antioxidant found in grapes and red wine. Also, it is a resveratrol analog with increased antiproliferative activity towards a number of cancer cell lines.
使用Resveratrol is a potent antioxidant found in grapes and red wine that also has anti-proliferative, anti-neoplastic and anti-angiogenic activities. In addition, resveratrol activates sirtuins and, in yeast, extends lifespan. cis-trismethoxy Resveratrol is a potent anti-mitotic drug that is 100-fold more active than resveratrol at inhibiting the growth of human colon cancer Caco-2 cells. It inhibits tubulin polymerization in a dose-dependent manner (IC50 = 4 μM) and inhibits enzymes involved in the synthesis of the polyamines, putrescine, and spermidine. trans-trismethoxy Resveratrol has superior pharmacokinetic characteristics when compared with resveratrol, including greater plasma exposure, longer elimination half-life, and lower clearance.
in vitrocis-trismethoxy resveratrol at 0.3 microm could exert a 80% growth inhibition of human colon cancer caco-2 cells and arrest growth completely at 0.4 microm. the cis conformation of cis-trismethoxy resveratrol was also 100-fold more potent than the trans isomer. cis-trismethoxy resveratrol was able to cause cell cycle arrest at the g2/m phase transition and inhibit tubulin polymerization dose-dependently, leading to the depletion of the polyamines, putrescine and spermidine. in addition, cis-trismethoxy resveratrol inhibited partially colchicine binding to its binding site on tubulin [1].
in vivoprevious study found that from the angle of pharmacokinetics, cis-trismethoxy resveratrol appeared to be a superior analog of resveratrol since it was orally available and showed greater plasma exposure, longer elimination half-life and lower clearance. due to the superior pharmacokinetic characteristics of cis-trismethoxy resveratrol had, its potentials as a preventive or therapeutic agent in resveratrol-effective diseases would be considered [2].
IC 504 microm for tubulin polymerization
参考文献[1] schneider, y. ,chabert, p.,stutzmann, j., et al. resveratrol analog (z)-3,5,4'-trimethoxystilbene is a potent anti-mitotic drug inhibiting tubulin polymerization. international journal of cancer 107, 189-196 (2003).
[2] lin, h. s. and ho, p.c. a rapid hplc method for the quantification of 3,5,4'-trimethoxy-trans-stilbene (tms) in rat plasma and its application in pharmacokinetic study. journal of pharmaceutical & biomedical analysis 49, 387-392 (2009).
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