CAS: 1414943-88-6; 4-(4-Fluoro-2-Methoxyphenyl)-N-(3-((S-Methylsulfonimidoyl)Methyl)Phenyl)-1,3,5-Triazin-2-Amine

该化合物是针对依赖环球的动脉(CDKs)的一个小分子抑制剂,专门为肿瘤学和细胞循环调节研究的研究应用而开发.作为一种种族混合物,它为调查CCDK抑制的立体化学影响提供了平衡的剖面,提供了结构活动关系的洞察力.它的主要优点包括:对CDK2和CDK9的高度抵抗力,使其成为研究癌症模型中转录规程和流行病的宝贵工具.种族成形形式允许与对应性衍生物进行比较研究,促进加深对动脉选择性和作用的手力影响的理解.它适合于体外和临床前的研究,它支持CDK依赖路径的机械探索.

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    主要参考文献


    1: Ruff JP, Kretz AL, Kornmann M, Henne-Bruns D, Lemke J, Traub B. The Novel, Orally Bioavailable CDK9 Inhibitor Atuveciclib Sensitises Pancreatic Cancer Cells to TRAIL-induced Cell Death. Anticancer Res. 2021 Dec;41(12):5973-5985. doi: 10.21873/anticanres.15416. 12(21):1776-1793. doi: 10.1002/cmdc.201700447. Epub 2017 Oct 16.
    3: Ni W, Zhang F, Zheng L, Wang L, Liang Y, Ding Y, Yik JHN, Haudenschild DR, Fan S, Hu Z. Cyclin-Dependent Kinase 9 (CDK9) Inhibitor Atuveciclib Suppresses Intervertebral Disk Degeneration via the Inhibition of the NF-κB Signaling Pathway. Front Cell Dev Biol. 2020 Sep 10;8:579658. doi: 10.3389/fcell.2020.579658.
    4: Brisard D, Eckerdt F, Marsh LA, Blyth GT, Jain S, Cristofanilli M, Horiuchi D, Platanias LC. Antineoplastic effects of selective CDK9 inhibition with atuveciclib on cancer stem-like cells in triple-negative breast cancer. Oncotarget. 2018 Dec 18;9(99):37305-37318. doi: 10.18632/oncotarget.26468.

    合成参考文献


    参考文献:10.1055/s-0041-1737909
    摘要:Dohi T, Zhdankin VV, Kumar R, Rimi R, Soni S, Uttam B, China H. Recyclable Hypervalent Iodine Reagents in Modern Organic Synthesis. Synthesis. 2022 Mar 23;54(12):2731–48. doi: 10.1055/s-0041-1737909.
    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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