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BGB-3111研究进展

发布日期：2017-10-30   浏览次数：0
核心提示：a href=https://www.medchemexpress.com/BGB-3111.htmlBGB-3111/a产品描述：BGB-3111 is a potent, selective and orally availa
<a href="https://www.medchemexpress.com/BGB-3111.html">BGB-3111</a>产品描述：BGB-3111 is a potent, selective and orally available Bruton's tyrosine kinase (<b>Btk</b>) inhibitor.

<i><b>In Vitro:</b></i> In both biochemical and cellular assays, BGB-3111 demonstrates nanomolar Btk inhibition activity. In several MCL and DLBCL cell lines, BGB-3111 inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. In comparison with ibrutinib, BGB-3111 shows much more restricted off-target activities against a panel of kinases, including ITK. BGB-3111 is at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity<sup>[1]</sup>.

<i><b>In Vivo:</b></i> BGB-3111 induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted either subcutaneously or systemically via tail vein injection in mice. In the subcutaneous xenografts. Preliminary 14-day toxicity study in rats shows that BGB-3111 is very well tolerated and <br><br>
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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/bgb-3111.html">www.medchemexpress.cn/bgb-3111.html</a><br><br></span><img style="width: 600.0px;height: 310.0px;"

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