GNE-274 | ER partial agonist | Probechem Biochemicals

Chemical Structure : GNE-274

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GNE-274 (GNE274)

货号: PC-73046Not For Human Use, Lab Use Only.

GNE-274 (GNE274) is a small molecule non-degrader, partial agonist of estrogen receptor (ER), failed to trigger increased ER turnover in tested cell line.

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生物&药学活性

GNE-274 (GNE274) is a small molecule non-degrader, partial agonist of estrogen receptor (ER), failed to trigger increased ER turnover in tested cell line.
GNE-274 potently inhibited cellular proliferation of ER+ HER2-negative cell lines, induced an LBD antagonist conformation similar to GDC-0927, neither promotes the degree of anti-proliferative activity achieved by GDC-0927.
GNE-274 displays considerable transcriptional agonism, GNE-274 increased chromatin accessibility at 373 induced ER binding site.

物理化学性质&存储条件

分子量	457.57
分子式	C29H31NO4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-3-(3-hydroxyphenyl)-4-methyl-2-(4-((1-propylazetidin-3-yl)methoxy)phenyl)-2H-chromen-6-ol

参考文献

1. Guan J, et al. Cell. 2019 Aug 8;178(4):949-963.e18.

GNE-274 (GNE274)

生物&药学活性

物理化学性质&存储条件

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GNE-274 (GNE274)

生物&药学活性

物理化学性质&存储条件

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