Endoxifen Z-isomer HCl is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen Z-isomer HCl inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM.
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Endoxifen Z-isomer hydrochloride, recognized as a pivotal Tamoxifen metabolite, plays a crucial role in delivering the anti-estrogenic effects of Tamoxifen in breast cancer cells that express estrogen receptor-alpha (ERα). It impedes hERG tail currents at 50 mV in a dose-responsive manner, with IC50 values established at 1.6 μM[1]. Furthermore, Endoxifen demonstrates greater potency in inhibiting estrogen target genes in the presence of ERβ. Notably, in patients treated with Tamoxifen exhibiting deficient CYP2D6 activity, low Endoxifen concentrations (20 to 40 nM) significantly reduce estrogen-induced cell proliferation rates when ERβ is expressed, contrasting with the higher concentrations required in the absence of ERβ[2].
Endoxifen Z-isomer HCl 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
MCF7 cells
10 uM
Function assay
6 h
Upregulation of ERalpha protein levels in human MCF7 cells at 10 uM after 6 hrs by Western blot method
24332630
MCF7:WS8 cells
Function assay
48 h
Agonist activity at ER in human MCF7:WS8 cells assessed as GREB1 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis
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