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Navitoclax研究进展

发布日期:2017-10-27   浏览次数:0
核心提示:a href=https://www.medchemexpress.com/navitoclax.htmlNavitoclax/a产品描述:Navitoclax is a potent and orally bioavailabl
<a href="https://www.medchemexpress.com/navitoclax.html">Navitoclax</a>产品描述:Navitoclax is a potent and orally bioavailable <b>Bcl-2 family protein</b> inhibitor that binds with high affinity (<b>K<sub>i</sub></b> < 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-x<sub>L</sub>, Bcl-2 and Bcl-w.

IC50 & Target: Ki: < 1 nM (Bcl-x<sub>L</sub>), < 1 nM (Bcl-2), < 1 nM (Bcl-w)

<i><b>In Vitro:</b></i> Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. The median IC<sub>50</sub> for all of the lines in the panel is 1.91 µM<sup>[1]</sup>. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation at all paclitaxel doses tested in both SK-OV-3 and IGROV-1 cell lines<sup>[2]</sup>.

<i><b>In Vivo:</b></i> Navitoclax (100 mg/kg/day, p.o.) also improves responses to bendamustine-rituximab (BR) in a subset of tumours in mice xenograft<sup>[3]</sup>.<br><br>
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