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CEP-40783研究進(jìn)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/CEP-40783.htmlCEP-40783/a產(chǎn)品描述：CEP-40783 is a potent, selective and orally ava
<a href="https://www.medchemexpress.com/CEP-40783.html">CEP-40783</a>產(chǎn)品描述：CEP-40783 is a potent, selective and orally available inhibitor of <b>AXL</b> and <b>c-Met</b> with <b>IC<sub>50</sub></b> values of 7 nM and 12 nM, respectively.

IC50 & Target: IC50: 7 nM (AXL) and 12 nM (c-Met)<sup>[1]</sup>

<i><b>In Vitro:</b></i> In AXL-transfected 293GT cells, CEP-40783 is 27-fold more active compared to recombinant enzyme with an IC<sub>50</sub> value of 0.26 nM. CEP-40783 also demonstrates superior activity against c-Met in GTL-16 cells (IC<sub>50</sub>=6 nM). The increased inhibitory activity of CEP-40783 in cells could be attributed to its extended residence time on both AXL and c-Met, consistent with a Type II mechanism. CEP-40783 shows high kinome selectivity against 298 kinases with an S90 of 0.04 (fraction of kinases showing >90% inhibition at 1 µM)<sup>[1]</sup>.

<i><b>In Vivo:</b></i> CEP-40783 shows dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with 80% target inhibition at 0.3 mg/kg 6 h post dose and co<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(kù)。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/cep-40783.html">www.medchemexpress.cn/cep-40783.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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