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CFI-402257研究進(jìn)展

發(fā)布日期：2017-10-30   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/CFI-402257.htmlCFI-402257/a產(chǎn)品描述：CFI-402257 is a highly selective and orally b
<a href="https://www.medchemexpress.com/CFI-402257.html">CFI-402257</a>產(chǎn)品描述：CFI-402257 is a highly selective and orally bioavailable <b>TTK</b> and <b>Mps1</b> inhibitor with <b>K<sub>i</sub></b>s of 0.1 and 0.09 nM, respectively.

IC50 & Target: Ki: 0.1 nM (TTK)<sup>[1]</sup>, 0.09 nM (Mps1)<sup>[2]</sup>; EC50: 6.5 nM (Mps1)<sup>[2]</sup>



<i><b>In Vitro:</b></i> CFI-402257 is highly selective to TTK. CFI-402257 is tested against a panel of human kinases at 1 μM and inhibits none of the 262 kinases tested. CFI-402257 is a potent inhibitor of cell growth<sup>[1]</sup>. CFI-402257 shows strong antineoplastic activity on a broad panel of human cancer-derived cell lines, and causes effects consistent with depletion or inhibition of Mps1. CFI-402257 inhibits Mps1 with an IC<sub>50</sub> value of 1.2 nM, and is ATP competitive with a K<sub>i</sub> value of 0.09 nM. CFI-402257 inhibits autophosphorylation of Mps1 at threonine 12/serine 15 with an EC<sub>50</sub> value of 6.5 nM in cells exogenously expressing human Mps1. CFI-402257 exerts potent growth inhibitor<br><br>
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已為全球多個(gè)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/cfi-402257.html">www.medchemexpress.cn/cfi-402257.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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