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Veliparib研究進(jìn)展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/Veliparib.htmlVeliparib/a產(chǎn)品描述：Veliparib is a potent bPARP/b inhibitor, inhibi
<a href="https://www.medchemexpress.com/Veliparib.html">Veliparib</a>產(chǎn)品描述：Veliparib is a potent <b>PARP</b> inhibitor, inhibiting <b>PARP1</b> and <b>PARP2</b> with <b>K<sub>i</sub></b>s of 5.2 and 2.9 nM, respectively.

IC50 & Target: Ki: 5.2 nM (PARP1), 2.9 nM (PARP2)<sup>[1]</sup>

<i><b>In Vitro:</b></i> Veliparib (ABT-888) is also tested against SIRT2, an enzyme that also uses NAD<sup>+</sup> for catalysis, and found to be inactive (>5,000 nM). The receptor profile of Veliparib is determined in a panel of 74 receptor-binding assays at a concentration of 10 μM. Veliparib displaces control-specific binding at 50% or greater at the human H<sub>1</sub>(61%), the human 5-HT<sub>1A</sub> (91%), and the human 5-HT<sub>7</sub> (84%) sites only. The IC<sub>50</sub>s for these three receptors are 5.3, 1.5, and 1.2 μM, respectively<sup>[1]</sup>. c-Met knockdown cells show 4.2- (shMet-A; 95% CI=4-4.5) or 4.6-fold (shMet-B; 95% CI=4.4-4.8) growth inhibition when treated with 60 μM Veliparib (ABT-888). When treated with 38 μM Veliparib, c-Met knockdown cells show 2<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(kù)。</span><br><br>產(chǎn)品鏈接：<a href="http://www.medchemexpress.cn/veliparib.html">www.medchemexpress.cn/veliparib.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"

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