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CHMFL-BMX-078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/CHMFL-BMX-078.htmlCHMFL-BMX-078/a产品描述：CHMFL-BMX-078 is a highly potent and se
<a href="https://www.medchemexpress.com/CHMFL-BMX-078.html">CHMFL-BMX-078</a>产品描述：CHMFL-BMX-078 is a highly potent and selective type II irreversible <b>BMX</b> kinase inhibitor with an <b>IC<sub>50</sub></b> of 11 nM.

IC50 & Target: IC50: 11 nM (BMX)<sup>[1]</sup>

<i><b>In Vitro:</b></i> Bone marrow kinase in the X chromosome (BMX, also called ETK) is a nonreceptor tyrosine kinase involved in tumorigenicity, cell motility, adhesion, angiogenesis, proliferation, and differentiation. CHMFL-BMX-078 exhibits an IC<sub>50</sub> of 11 nM by formation of a covalent bond with cysteine 496 residue in the DFG-out inactive conformation of BMX. It displays a high selectivity profile against the 468 kinases/mutants in the KINOMEscan evaluation and achieves at least 40-fold selectivity over BTK kinase (IC<sub>50</sub>=437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding K<sub>d</sub> of 81 nM, while for the active state of BMX kinase, it exhibits a binding K<sub>d</sub> of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX c<br><br>
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