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Acelarin研究進展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/Acelarin.htmlAcelarin/a產品描述：Acelarin (NUC-1031) is a ProTide transformation a
<a href="https://www.medchemexpress.com/Acelarin.html">Acelarin</a>產品描述：Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.


IC50 & Target: EC50：0.2 nM (DNA synthesis inhibitor)<sup>[1]</sup>

<i><b>In Vitro:</b></i> Gemcitabine is a nucleoside analogue commonly used in cancer therapy but with limited efficacy due to a high susceptibility to cancer cell resistance. The addition of a phosphoramidate motif to the gemcitabine can protect it against many of the key cancer resistance mechanisms. A series of gemcitabine phosphoramidate prodrugs are synthesized and screened for cytostatic activity in a range of different tumor cell lines. Among the synthesized compounds, NUC-1031 is shown to be potent <i>in vitro</i>.

<i><b>In Vivo:</b></i> The ProTide demonstrates a significant reduction in tumor size against pancreatic xenograft models compared with the gemcitabine treated group, and less adverse effects on body weight, indicating a better safety profile. Data strongly suggests that the ProTi<br><br>
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已為全球多個知名企業(yè)、院校構建各種定制型化合物庫。</span><br><br>產品鏈接：<a href="http://www.medchemexpress.cn/acelarin.html">www.medchemexpress.cn/acelarin.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

src="http://img.dxycdn.com/trademd/upload/userfiles/image/2014/08/A1408605159png_small.jpg"

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