CAS: 1410880-22-6; 3-(4-(Dimethylamino)But-2-Enamido)-N-(3-Methyl-4-((4-(Pyridin-3-yl)Pyrimidin-2-yl)Amino)Phenyl)Benzamide

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    专利号:US-2025049791-A1
    优先权日:2023-08-03
    标题:Synthesis of MEK7 Inhibitors and methods of Use Thereof
    发明人:SCHEIDT KARL A; KIM DALTON ROBERT; ORR MEGHAN JO
    权利人:UNIV NORTHWESTERN
    摘要:Disclosed herein are 4-phenoxypyrimidine compounds and derivatives thereof for use as inhibitors of mitogen-activated protein kinase 7 (MEK7). The disclosed compounds and pharmaceutical compositions thereof may be used in methods for treating a disease or disorder associated with MEK7 activity, including cell proliferative diseases and disorders associated with MEK7 activity, such as cancer.

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    主要参考文献


    1: Xie X, Kaoud TS, Edupuganti R, Zhang T, Kogawa T, Zhao Y, Chauhan GB, Giannoukos DN, Qi Y, Tripathy D, Wang J, Gray NS, Dalby KN, Bartholomeusz C, Ueno NT. c-Jun N-terminal kinase promotes stem cell phenotype in triple-negative breast cancer through upregulation of Notch1 via activation of c-Jun. Oncogene. 2016 Dec 12. doi: 10.1038/onc.2016.417. [Epub ahead of print] doi: 10.1016/j.brainres.2016.10.013. doi: 10.1016/j.chembiol.2011.11.010.
    4: Pathria G, Garg B, Garg K, Wagner C, Wagner SN. Dual c-Jun N-terminal kinase-cyclin D1 and extracellular signal-related kinase-c-Jun disjunction in human melanoma. Br J Dermatol. 2016 Dec;175(6):1221-1231. doi: 10.1111/bjd.14713. doi: 10.1016/j.bbrc.2013.09.130.

    合成参考文献


    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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