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PD-166866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/PD166866.htmlPD-166866/a产品描述：PD166866 is a selective bFGFR/b tyrosine kinase
<a href="https://www.medchemexpress.com/PD166866.html">PD-166866</a>产品描述：PD166866 is a selective <b>FGFR</b> tyrosine kinase inhibitor with an <b>IC<sub>50</sub></b> of 52.4 nM.

IC50 & Target: IC50: 52.4 nM (hFGFR tyrosine kinase)<sup>[1]</sup>

<i><b>In Vitro:</b></i> PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC<sub>50</sub> value of 52.4 nM and is characterized as an ATP competitive inhibitor of the FGFR-1. PD 166866 is a potent inhibitor of FGFR autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase. PD 166866 also inhibits bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms in L6 cells. Daily exposure of PD 166866 to L6 cells at concentrations from 1 to 100 nM results in a concentration-related inhibition of bFGF-stimulated cell growth for 8 consecutive days with an IC<sub>50</sub> value of 24 nM<sup>[1]</sup>.

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