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LY3214996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/LY3214996.htmlLY3214996/a產(chǎn)品描述：LY3214996 is a highly selective inhibitor of bE
<a href="https://www.medchemexpress.com/LY3214996.html">LY3214996</a>產(chǎn)品描述：LY3214996 is a highly selective inhibitor of <b>ERK1</b> and <b>ERK2</b>, with <b>IC<sub>50</sub></b> of 5 nM for both enzymes in biochemical assays.

IC50 & Target: IC50: 5 nM (ERK1/2)<sup>[1]</sup>

<i><b>In Vitro:</b></i> LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC<sub>50</sub> of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to LY3214996<sup>[1]</sup>.

<i><b>In Vivo:</b></i> In tumor xenograft models, LY3214996 inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities. LY3214996 shows either similar or superior anti-tumor activity as compared to other published ERK inhibitors in BRAF or RAS mutant c<br><br>
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<span style="outline: 0.0px;line-height: 22.0px;color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;background-color: rgb(251,251,251);">公司介紹：MedChemExpress(MCE)專注于各種抑制劑、激動(dòng)劑、API及化合物庫，總部位于美國新澤西，分別在瑞典和上海設(shè)有歐洲區(qū)子公司和亞洲區(qū)總代理，營銷網(wǎng)點(diǎn)遍及全球20多個(gè)國家地區(qū)。MCE經(jīng)過多年努力已成為全球生物活性小分子領(lǐng)域的一流供應(yīng)商， 產(chǎn)品涵蓋癌癥、神經(jīng)科學(xué)、抗感染、表觀遺傳學(xué)等20個(gè)熱門研究領(lǐng)域，PI3K、MAPK等近千個(gè)細(xì)分靶點(diǎn)，超過4000個(gè)活性小分子化合物現(xiàn)貨，以及GPCR、API、離子通道等超過20種不同類型的化合物庫，同時(shí)提供從毫克到千克的專業(yè)定制合成服務(wù)。</span>
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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/ly3214996.html">www.medchemexpress.cn/ly3214996.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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