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ARV-771研究進展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/ARV-771.htmlARV-771/a產(chǎn)品描述：ARV-771 is a potent bromodomain and extra-terminal
<a href="https://www.medchemexpress.com/ARV-771.html">ARV-771</a>產(chǎn)品描述：ARV-771 is a potent bromodomain and extra-terminal (<b>BET</b>) proteins degrader with <b>K<sub>d</sub></b> values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively.

IC50 & Target: Kd: 4.7 (BRD 2), 7.6 (BRD 3), 7.6 nM (BRD 4)<sup>[1]</sup>

IC50: less than 1 nM (c-MYC protein)<sup>[1]</sup>



<i><b>In Vitro:</b></i> ARV-771 potently degrades BRD2/3/4 in 22Rv1 cells with a DC<sub>50</sub> less than 5 nM. c-MYC protein is a downstream effector of BET proteins. Treatment with ARV-771 results in depletion of c-MYC with an IC<sub>50</sub> of less than 1 nM. ARV-771 shows strong antiproliferative effect on 22Rv1, VCaP, and LnCaP95 cell lines. ARV-771 treatment has a pronounced effect on cell morphology consistent with apoptosis. FL-AR and AR-V7 mRNA are down-regulated upon treatment with 10 nM ARV-771 in VCaP cells. ARV-771 has an antiandrogenic effect on a number of AR-regulated genes in VCaP cells<sup>[1]</sup>.

<i><b>In Vivo:</b></i> Treatment of non castrated male Nu/N<br><br>
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