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CHMFL-BMX-078研究進展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/CHMFL-BMX-078.htmlCHMFL-BMX-078/a產(chǎn)品描述：CHMFL-BMX-078 is a highly potent and se
<a href="https://www.medchemexpress.com/CHMFL-BMX-078.html">CHMFL-BMX-078</a>產(chǎn)品描述：CHMFL-BMX-078 is a highly potent and selective type II irreversible <b>BMX</b> kinase inhibitor with an <b>IC<sub>50</sub></b> of 11 nM.

IC50 & Target: IC50: 11 nM (BMX)<sup>[1]</sup>

<i><b>In Vitro:</b></i> Bone marrow kinase in the X chromosome (BMX, also called ETK) is a nonreceptor tyrosine kinase involved in tumorigenicity, cell motility, adhesion, angiogenesis, proliferation, and differentiation. CHMFL-BMX-078 exhibits an IC<sub>50</sub> of 11 nM by formation of a covalent bond with cysteine 496 residue in the DFG-out inactive conformation of BMX. It displays a high selectivity profile against the 468 kinases/mutants in the KINOMEscan evaluation and achieves at least 40-fold selectivity over BTK kinase (IC<sub>50</sub>=437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding K<sub>d</sub> of 81 nM, while for the active state of BMX kinase, it exhibits a binding K<sub>d</sub> of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX 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)、院校構建各種定制型化合物庫。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/chmfl-bmx-078.html">www.medchemexpress.cn/chmfl-bmx-078.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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