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10074-G5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/10074-G5.html10074-G5/a產(chǎn)品描述：10074-G5 is an inhibitor of bc-Myc-Max/b dimeriza
<a href="https://www.medchemexpress.com/10074-G5.html">10074-G5</a>產(chǎn)品描述：10074-G5 is an inhibitor of <b>c-Myc-Max</b> dimerization with an <b>IC<sub>50</sub></b> of 146 μM.

IC50 & Target: IC50: 15.6 μM (Daudi cells), 13.5 μM (HL-60 cells)<sup>[1]</sup>, 146 μM (c-Myc–Max)<sup>[2]</sup>

<i><b>In Vitro:</b></i> 10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disruptes c-Myc/Max dimerization. The <b>IC<sub>50</sub></b> values against Daudi and HL-60 cells are 15.6 and 13.5 μM, respectively<sup>[1]</sup>. 10074-G5 binds the Myc peptide Myc353-437 with a K<sub>d</sub> value of 2.8 μM in the region Arg363-Ile381. 10074-G5 binds in a cavity that is created by a kink (Asp379-Ile381) in the N-terminus of an induced helical domain (Leu370–Arg378)<sup>[3]</sup>.

<i><b>In Vivo:</b></i> The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration was 58 μM, which is 10-fold higher than peak tumor concentration<sup>[1]</sup>.<br><br>
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已為全球多個知名企業(yè)、院校構(gòu)建各種定制型化合物庫。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/10074-g5.html">www.medchemexpress.cn/10074-g5.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

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