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Pan-RAS-IN-1研究進展

發(fā)布日期：2017-10-27   瀏覽次數：0
核心提示：a href=https://www.medchemexpress.com/Pan-RAS-IN-1.htmlPan-RAS-IN-1/a產品描述：Pan-RAS-IN-1 is a bpan-Ras/b inhibitor th
<a href="https://www.medchemexpress.com/Pan-RAS-IN-1.html">Pan-RAS-IN-1</a>產品描述：Pan-RAS-IN-1 is a <b>pan-Ras</b> inhibitor that disrupts the interaction of Ras proteins and their effectors.

<i><b>In Vitro:</b></i> Pan-RAS-IN-1 binds to KRas<sup>G12D</sup>-GppNHp with an affinity less than 20 μM. Pan-RAS-IN-1 binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins. The potency of pan-RAS-IN-1 correlates with the degree of dependency on the mutated isoform over a 5-fold concentration range. At some concentrations, pan-RAS-IN-1 is cytostatic, possibly due to pan-RAS inhibition. Pan-RAS-IN-1 is evaluated in primary T cell acute lymphoblastic leukemia (T-ALL) cells. Selective lethality is observed, with mutant NRAS cells retaining only 20%-40% viability after 5 μM treatment<sup>[1]</sup>.



<i><b>In Vivo:</b></i> Pan-RAS-IN-1 administration results in inhibition of tumor growth over 15 days of treatment. Pan-RAS-IN-1-treated mice exhibits decreased tumor pERK levels compared with vehicle treated mice. A modest increase<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/pan-ras-in-1.html">www.medchemexpress.cn/pan-ras-in-1.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

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