http://www.pathway2curis.com/cu-906-inhibitor-hdac-and-pi3k-mtor-f17.html CU-906 is a multi-targeted molecule that is designed to inhibit HDAC and PI3K and mTOR kinases, the combination of which Curis scientists believe have synergistic interaction against cancer cells. In vitro mechanism of action studies demonstrated that CU-906 is able to inhibit Class I PI3K and mTOR kinases, suppress multiple nodes of other survival pathways including the RAF-MEK-ERK pathway, and upregulate P21, which is a cyclin-dependent kinase inhibitor that can promote cancer cell death when upregulated. The suppression of non-PI3K-AKT-mTOR survival pathways occurs via epigenetic modification as a result of the inhibition of HDAC, the non-kinase target of CU-906. By contrast, single-target PI3K inhibitors and PI3K/mTor dual inhibitors that only target the primary PI3K and/or mTOR kinase survival pathways, have only been shown to have limited effects on tumors with disregulation of other signaling pathways.<br /><br />CU-906 exhibits anti-proliferation activity against a broad range of cancer cell types in in vitro studies, including cell lines that are insensitive to PI3K inhibitors. CU-906's anti-proliferation activity is up to 100 times more potent than that of two leading PI3K inhibitors in development. Efficacy studies in various K-RAS mutant tumor xenograft models indicate that this compound has more potent antitumor activity than a leading PI3K inhibitor that is currently in clinical development, at doses causing no obvious side effects to the tumor-bearing animals.<br /><br />Importantly, CU-906 displays high exposure and long half-life in tumor tissue after IV administration and is orally bioavailable in preclinical models. CU-906 has a half-life of more than 10 hours in xenograft tumors, induces apoptosis and inhibits cell proliferation up to 48 hours following a single dose of the compound to tumor-bearing animals. <b>Statistics</b> : 1 Topics || 2 Posts Last post by <span style="color: #AA0000;" class="username-coloured">hedgehog</span> Fri, 10 Dec 2010 01:54:25 GMT http://www.pathway2curis.com/gym_sitemaps/images/rss_forum_big.gif http://www.pathway2curis.com/cu-906-inhibitor-hdac-and-pi3k-mtor-f17.html http://blogs.law.harvard.edu/tech/rss Google Yahoo MSN Sitemaps and RSS 2.0.0 - © 2006, 2007, 2008 www.phpBB-SEO.com 6 CU-906 is a multi-targeted molecule that is designed to inhibit HDAC and PI3K and mTOR kinases, the combination of which Curis scientists believe have synergistic interaction against cancer cells. In vitro mechanism of action studies demonstrated that CU-906 is able to inhibit Class I PI3K and mTOR kinases, suppress multiple nodes of other survival pathways including the RAF-MEK-ERK pathway, and upregulate P21, which is a cyclin-dependent kinase inhibitor that can promote cancer cell death when upregulated. The suppression of non-PI3K-AKT-mTOR survival pathways occurs via epigenetic modification as a result of the inhibition of HDAC, the non-kinase target of CU-906. By contrast, single-target PI3K inhibitors and PI3K/mTor dual inhibitors that only target the primary PI3K and/or mTOR kinase survival pathways, have only been shown to have limited effects on tumors with disregulation of other signaling pathways.<br /><br />CU-906 exhibits anti-proliferation activity against a broad range of cancer cell types in in vitro studies, including cell lines that are insensitive to PI3K inhibitors. CU-906's anti-proliferation activity is up to 100 times more potent than that of two leading PI3K inhibitors in development. Efficacy studies in various K-RAS mutant tumor xenograft models indicate that this compound has more potent antitumor activity than a leading PI3K inhibitor that is currently in clinical development, at doses causing no obvious side effects to the tumor-bearing animals.<br /><br />Importantly, CU-906 displays high exposure and long half-life in tumor tissue after IV administration and is orally bioavailable in preclinical models. CU-906 has a half-life of more than 10 hours in xenograft tumors, induces apoptosis and inhibits cell proliferation up to 48 hours following a single dose of the compound to tumor-bearing animals. <b>Statistics</b> : 1 Topics || 2 Posts Last post by <span style="color: #AA0000;" class="username-coloured">hedgehog</span>RSS 2.0 feed link http://www.pathway2curis.com/cu-906-inhibitor-hdac-and-pi3k-mtor-f17/news/forum.xml gym_sitemaps http://www.pathway2curis.com/cu-906-preclinical-information-t24.html Tue, 07 Dec 2010 01:52:09 GMT <h5><a href="http://www.pathway2curis.com/cu-906-inhibitor-hdac-and-pi3k-mtor-f17.html" title="CU-906 (Inhibitor HDAC and PI3K/mTOR)">CU-906 (Inhibitor HDAC and PI3K/mTOR)</a></h5> <b>Statistics</b> : 2 Post || 432 Views Post by <span style="color: #AA0000;" class="username-coloured">hedgehog</span> hedgehog CU-906 (Inhibitor HDAC and PI3K/mTOR) - News http://www.pathway2curis.com/cu-906-preclinical-information-t24.html