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BI-9564

發(fā)布日期：2017-10-26   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/BI-9564.htmlBI-9564/a產(chǎn)品描述：BI-9564 is a selective, and cell-permeable bBRD9 BD
<a href="https://www.medchemexpress.com/BI-9564.html">BI-9564</a>產(chǎn)品描述：BI-9564 is a selective, and cell-permeable <b>BRD9 BD</b> inhibitor, with K<sub>d</sub> of 5.9 nM for BRD9, and IC<sub>50</sub> of > 100 μM for BET family.

IC50 & Target: Kd: 20 nM (BRD9)

<i><b>In Vitro:</b></i> BI-9564 (<5 μM) shows no activity against 324 kinases, and at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC<sub>50</sub> of 800 nM<sup>[1]</sup>. BI-9564 shows K<sub>d</sub> of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells<sup>[2]</sup>.

<i><b>In Vivo:</b></i> BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for in vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML<su<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(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個熱門研究領(lǐng)域，PI3K、MAPK等近千個細(xì)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(wù)。</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/bi-9564.html">www.medchemexpress.cn/bi-9564.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"

alt="">
 
 
 
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