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cis-trismethoxy Resveratrol

(Synonyms: 顺式白藜芦醇三甲醚,cis-Trimethoxy Stilbene) 目录号 : GC12352

Potent antineoplastic agent

cis-trismethoxy Resveratrol Chemical Structure

Cas No.:94608-23-8

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10mg
¥168.00
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50mg
¥756.00
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100mg
¥1,344.00
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500mg
¥5,880.00
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Sample solution is provided at 25 µL, 10mM.

Description

IC50: 4 microM for tubulin polymerization

cis-trismethoxy Resveratrol is an anti-mitotic drug.

A mitotic inhibitor is a drug inhibiting mitosis or cell division. Mitotic inhibitors are widely used in cancer treatment, because cancer cells can grow and eventually spread through the body via continuous mitotic division.

In vitro: cis-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 vivo: Previous 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].

Clinical trial: So far, no clinical study has been conducted.

References:
[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).

化学性质

Cas No. 94608-23-8 SDF
别名 顺式白藜芦醇三甲醚,cis-Trimethoxy Stilbene
化学名 1,3-dimethoxy-5-[(1Z)-2-(4-methoxyphenyl)ethenyl]-benzene
Canonical SMILES COC1=CC(/C=C\C2=CC=C(OC)C=C2)=CC(OC)=C1
分子式 C17H18O3 分子量 270.3
溶解度 ≤50mg/ml in DMSO;50mg/ml in dimethyl formamide 储存条件 Store at -20°C
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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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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.6996 mL 18.498 mL 36.9959 mL
5 mM 0.7399 mL 3.6996 mL 7.3992 mL
10 mM 0.37 mL 1.8498 mL 3.6996 mL
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