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      SHP099 (hydrochloride)

      發(fā)布日期:2017-10-26   瀏覽次數(shù):0
      核心提示:a href=https://www.medchemexpress.com/SHP099-hydrochloride.htmlSHP099 (hydrochloride)/a產(chǎn)品描述:SHP099 hydrochloride is
      <a href="https://www.medchemexpress.com/SHP099-hydrochloride.html">SHP099 (hydrochloride)</a>產(chǎn)品描述:SHP099 hydrochloride is a potent, selective, orally available <b>SHP2</b> inhibitor with an <b>IC<sub>50</sub></b> of 70 nM.

      IC50 & Target: IC50: 70 nM (SHP2)<sup>[1]</sup>

      <i><b>In Vitro:</b></i> The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with the basic amine and the Phe113 backbone carbonyl. SHP099 shows inhibition of cell proliferation (KYSE-520 model) with an IC<sub>50</sub> of 1.4 μM. SHP099 shows high solubility and high permeability with no apparent efflux in Caco-2 cells<sup>[1]</sup>. SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells<sup>[2]</sup>.



      <i><b>In Vivo:</b></i> After a single doses of 30 and 100 mg/kg (red and blue lines, respectively), dose-dependent exposure and modulation of the ph<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>
      <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 對每批產(chǎn)品都進行嚴格的LCMS和NMR檢驗,其產(chǎn)品已被全球近萬名客戶廣泛使用并發(fā)表大量文章、專利;</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);">
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      <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小時內(nèi)送達客戶;</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)品提供免費試用裝;</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/shp099-hydrochloride.html">www.medchemexpress.cn/shp099-hydrochloride.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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