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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>
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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。</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;"

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