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TAK-659 (hydrochloride)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/TAK-659_hydrochloride.htmlTAK-659 (hydrochloride)/a产品描述：TAK-659 hydrochloride
<a href="https://www.medchemexpress.com/TAK-659_hydrochloride.html">TAK-659 (hydrochloride)</a>产品描述：TAK-659 hydrochloride is a potent, selective and orally available spleen tyrosine kinase (<b>Syk</b>) with an <b>IC<sub>50</sub></b> of 3.2 nM.

IC50 & Target: IC50: 3.2 nM (Syk)<sup>[1]</sup>

<i><b>In Vitro:</b></i> In a cell proliferation assay, TAK-659 shows inhibition toward a SYK-dependent cell line (OCILY10). TAK-659 is shown to be sensitive toward FLT3-ITD dependent cell lines, MV4-11 and MOLM-13 while the WT FLT3 RS4-11 (ALL cell line) and RA1 (Burkitt’s Lymphoma cell line) are not sensitive toward TAK-659. The sensitivity to TAK-659 is associated with mutations impacting SYK activity in B cell lymphomas, wheras TAK-659 is not cytotoxic for adherent primary or solid tumor cell lines<sup>[1]</sup>. TAK-659 inhibits the microenvironment-induced activation of Syk and downstream signaling molecules, without inhibiting the protein homologue ZAP-70 in T cells. importantly, the pro-survival, proliferative, chemoresistant and activation effects promoted by the microenvironment are a<br><br>
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