Z6·尊龙凯时「中国」官方网站z6尊龙

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    中国：

    Email: marketing@kangtya.com

    业务咨询专线：400-780-8018

    （仅限服务咨询，其他事宜请拨打川沙总部电话）

    川沙总部电话: +86 (21) 5859-1500

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    0044 7790 816 954 (Europe)

    Email:marketing@medicilon.com
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XY153是一种有潜力的先导化合物，可用于开发针对急性髓系白血病。XY153在体外具有良好的代谢稳定性。所有肝微粒体测定均通过z6尊龙进行

2023-07-06
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Pan-bromodomain and extra terminal (Pan-BET) inhibitors show profound efficacy but exhibit pharmacology-driven toxicities in clinical trials. The representative Compound 8l (XY153), a novel BD2-selective BET inhibitor, potently binds to BRD4 BD2 with an IC50 value of 0.79 nM. XY153 displayed potent antiproliferative activity against multiple tumor cell lines. XY153 also demonstrated good metabolic stability in vitro. These data indicate that XY153 may serve as a new and valuable lead compound for the development of potential therapeutics against acute myeloid leukemia (AML). All liver microsome assays were performed by Medicilon. 

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Reference:

Junhua Li, et al. Structure-Based Discovery and Optimization of Furo[3,2- c]pyridin-4(5 H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors. J Med Chem. 2022 Apr 14;65(7):5760-5799. doi: 10.1021/acs.jmedchem.2c00100. 

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