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Afuresertib研究进展

发布日期：2017-10-31   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/Afuresertib.htmlAfuresertib/a产品描述：Afuresertib is an orally available, ATP-com
<a href="https://www.medchemexpress.com/Afuresertib.html">Afuresertib</a>产品描述：Afuresertib is an orally available, ATP-competitive, <b>pan-AKT</b> inhibitor with <b>K<sub>i</sub></b> of 0.08, 2 and 2.6 nM against <b>AKT1</b>, <b>AKT2</b> and <b>AKT3</b>, respectively.IC50 & Target: Ki: 0.08 nM (AKT1), 2 nM (AKT2), 2.6 nM (AKT3)<sup>[1]</sup><br/>IC50: 0.2 nM (AKT1<sup>E17K</sup>), 1.3 nM (PKA), 0.9 nM (PKG1α), 4 nM (PKG1β)<sup>[1]</sup><i><b>In Vitro:</b></i> Afuresertib (GSK2110183) shows concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both BT474 and LNCaP cell lines. GSK2110183 consistently has potent anti-proliferative effects on a variety of hematological malignancies. Overall 65% of the hematological cell lines are sensitive to GSK2110183 (EC<sub>50</sub><1 µM). Among solid tumor cell lines, 21% have EC<sub>50</sub><1 µM in response to GSK2110183<sup>[1]</sup>. <i><b>In Vivo:</b></i> Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK<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);">公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。</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 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、专利；</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 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足最新的科研需求；</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);">数千种产品在上海有充足备货，24-48小时内送达客户；</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);">大量产品提供免费试用装；</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);">已为全球多个知名企业、院校构建各种定制型化合物库。</span><br><br>产品链接：<a href="http://www.medchemexpress.cn/afuresertib.html">www.medchemexpress.cn/afuresertib.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="">