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ANI-7 是一种 AhR 途径的激活剂。ANI-7 抑制多种癌细胞的生长,并有选择地抑制 MCF-7 乳腺癌细胞的生长,GI50 为 0.56 μM。ANI-7 通过激活 AhR 途径诱导 CYP1 代谢单加氧酶,并在敏感的乳腺癌细胞系中诱导 DNA 损伤,检查点激酶 (Chk2) 激活,S 期细胞周期停滞和细胞死亡。
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines[1][2][3].
[1]. ilbert J, et al. (Z)-2-(3,4-Dichlorophenyl)-3-(1H-Pyrrol-2-yl)Acrylonitrile Exhibits Selective Antitumor Activity in Breast Cancer Cell Lines via the Aryl Hydrocarbon Receptor Pathway. Mol Pharmacol. 2018 Feb;93(2):168-177. [2]. Baker JR, et al. Dichlorophenylacrylonitriles as AhR Ligands That Display Selective Breast Cancer Cytotoxicity in vitro. ChemMedChem. 2018 Jul 18;13(14):1447-1458. [3]. Mark Tarleton, et al. Library synthesis and cytotoxicity of a family of 2-phenylacrylonitriles and discovery of an estrogen dependent breast cancer lead compound. ?Medicinal Chemistry Communication. January 20112. (1):31-37.
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