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IT1t前沿研究進(jìn)展

發(fā)布日期：2017-11-13   瀏覽次數(shù)：0
核心提示：IT1t是高效的bCXCR4/b拮抗劑；抑制CXCL12/CXCR4相互作用的bICsub50/sub/b值為2.1 nM。BRa href=https://www.medchemexpress.cn/B
IT1t是高效的<b>CXCR4</b>拮抗劑；抑制CXCL12/CXCR4相互作用的<b>IC<sub>50</sub></b>值為2.1 nM。<BR><a href="https://www.medchemexpress.cn/BAY1125976.html">BAY1125976</a>產(chǎn)品描述：BAY1125976 is a selective allosteric <b> Akt1/2</b> inhibitor; inhibits Akt1 and Akt2 activity with <b>IC<sub>50</sub></b> values of 5.2 nM and 18 nM at 10 μM ATP, respectively.IC50 & Target: IC50: 5.2 nM (Akt1, at 10 μM ATP), 18 nM (Akt2, at 10 μM ATP)<sup>[1]</sup><i><b>In Vitro:</b></i> BAY 1125976 is equally potent against Akt1 (IC<sub>50</sub>=5.2 nM at 10 μM ATP and 44 nM at 2 mM ATP)and Akt2(IC<sub>50</sub>=18 nM at 10 μM ATP and 36 nM at 2 mM ATP) isoforms and up to 86 fold less potent against Akt3 (IC<sub>50</sub>=427 nM at 10 μM ATP). It inhibits the Akt1 and Akt2 by binding into an allosteric binding pocket formed by kinase and PH domain. It inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors. It effectively blocks Akt signaling by inhibiting the phosphorylation of Akt and the downstream effectors, including eukaryotic translation initiation factor 4E b<br><br><br><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(zhuān)注于各種抑制劑、激動(dòng)劑、API及化合物庫(kù)，總部位于美國(guó)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(yíng)銷(xiāo)網(wǎng)點(diǎn)遍及全球20多個(gè)國(guó)家地區(qū)。MCE經(jīng)過(guò)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(mén)研究領(lǐng)域，PI3K、MAPK等近千個(gè)細(xì)分靶點(diǎn)，超過(guò)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(guò)20種不同類(lèi)型的化合物庫(kù)，同時(shí)提供從毫克到千克的專(zhuān)業(yè)定制合成服務(wù)。</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">MCE 對(duì)每批產(chǎn)品都進(jìn)行嚴(yán)格的LCMS和NMR檢驗(yàn)，其產(chǎn)品已被全球近萬(wàn)名客戶廣泛使用并發(fā)表大量文章、專(zhuān)利；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">MCE 定期增加各領(lǐng)域熱門(mén)抑制劑、激動(dòng)劑，不斷擴(kuò)增已有化合物庫(kù)，以滿足最新的科研需求；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">數(shù)千種產(chǎn)品在上海有充足備貨，24-48小時(shí)內(nèi)送達(dá)客戶；</span><br style="color: rgb(62,62,62);font-family: "Helvetica Neue" , Helvetica , Arial , sans-serif;font-size: 11.818182px;line-height: 22.0px;background-color: rgb(251,251,251);"><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);">大量產(chǎn)品提供免費(fèi)試用裝；</span><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);">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/BAY1125976.html">www.medchemexpress.cn/BAY1125976.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="">Purity:98%<BR>MWt:406.6515<BR>Formula:C21H34N4S2<BR>SMILES:CC1(C)CN2C(CS/C(NC3CCCCC3)=N\C4CCCCC4)=CSC2=N1<BR>Pathway:GPCR/G Protein; Immunology/Inflammation; <BR>Mechanisms:CXCR; <BR>Research Area:Inflammation/Immunology<BR>電話： 021-58955995<BR>網(wǎng)址： www.MedChemExpress.cn <BR>地址： 上海市浦東新區(qū)蔡倫路720號(hào)2號(hào)樓3層
 
 
 
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