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IPI549

發(fā)布日期：2017-10-26   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/IPI549.htmlIPI549/a產(chǎn)品描述：IPI549 is a potent and selective bPI3K/b Inhibitor wi
<a href="https://www.medchemexpress.com/IPI549.html">IPI549</a>產(chǎn)品描述：IPI549 is a potent and selective <b>PI3Kγ</b> Inhibitor with <b>IC<sub>50</sub></b> of 16 nM.

IC50 & Target: IC50: 16 nM (PI3Kγ), 3.2 μM (PI3Kα), 3.5 μM (PI3Kβ), >8.4 μM (PI3Kδ)<sup>[1]</sup>

<i><b>In Vitro:</b></i> IPI-549 inhibits PI3Kγ with IC<sub>50</sub> of 16 nM, with >100-fold selectivity over other lipid and protein kinases (PI3Kα IC<sub>50</sub>=3.2 μM, PI3Kβ IC<sub>50</sub>=3.5 μM, PI3Kδ IC<sub>50</sub>>8.4 μM). IPI549 is evaluated for activity across all Class I PI3K isoforms. The binding affinity of IPI549 for PI3K-γ is determined by measuring the individual rates constants and for PI3K-α, β and δ using equilibrium fluorescent titration. IPI549 is found to be a remarkably tight binder to PI3Kγ with a K<sub>d</sub> of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms (PI3Kα K<sub>d</sub>=17 nM, PI3Kβ K<sub>d</sub>=82 nM, PI3Kδ K<sub>d</sub>=23 M). In PI3K-α, -β, -γ, and -δ dependent cellular phospho-AKT assays, IPI549 demonstrates excellent PI3K-γ potenc<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)點遍及全球20多個國家地區(qū)。MCE經(jīng)過多年努力已成為全球生物活性小分子領(lǐng)域的一流供應商， 產(chǎn)品涵蓋癌癥、神經(jīng)科學、抗感染、表觀遺傳學等20個熱門研究領(lǐng)域，PI3K、MAPK等近千個細分靶點，超過4000個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，同時提供從毫克到千克的專業(yè)定制合成服務。</span>
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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/ipi549.html">www.medchemexpress.cn/ipi549.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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