GNE-274
目录号: PL03942 纯度: ≥98%
CAS No. :2369048-69-9
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中文名称
GNE-274
英文名称
GNE-274
英文别名
2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)-;GNE-274
Cas No.
2369048-69-9
分子式
C29H31NO4
分子量
457.56
包装储存
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
产品详情
GNE-274 是 ER 降解剂 GDC-0927 的结构类似物,是一种非降解剂。GNE-274 在乳腺癌细胞系中不诱导 ER 的转换,作为 ER 的部分激动剂 (partial ER agonist) 发挥作用。GNE-274 增加了ER-DNA 结合位点的的染色质可进入性,而 GDC-0927 则没有。GNE-274 是一种有效的 ER 配体结合域 (LBD) 抑制剂。GNE-274 可用于癌症研究。
生物活性
GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research.
性状
Solid
体外研究(In Vitro)
GNE-274 (0.1 nM-1000 nM; 4 hours) fails to trigger increased ER turnover in MCF7, MD-134, HCC1500 and CAMA cells.
GNE-274 (1-1000 nM; 7-10 days) potently inhibits cellular proliferation, exhibiting greater potency than fulvestrant, 4-OHT, AZD9496, and GDC-0810 in E2-stimulated ER breast cancer cell lines.
In transposaseaccessible chromatin sequencing (ATAC-seq) assay, GNE-274 increase chromatin accessibility at ER-DNA binding sites, it significantly alters chromatin accessibility at 594 sites. But GDC-0927 has considerably less impact on chromatin accessibility.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[1]. Jane Guan, et al. Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility. Cell. 2019 Aug 8;178(4):949-963.e18.
[2]. Jane Guan, et al. Abstract NG05: Not all “SERDs” are equal: Context-independent ER degradation and full ER antagonism define the next generation of ER therapeutics. Cancer research.
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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