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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Estrogen Receptor/ERR-GNE-149
GNE-149

Chemical Structure : GNE-149

CAS No.: 1953132-75-6

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GNE-149 (GNE149)

货号: PC-20524Not For Human Use, Lab Use Only.

GNE-149 (GNE149) is a potent, full estrogen receptor alpha (ERα) antagonist and degrader with IC50 of 0.053 nM (MCF7, ERα degradation).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GNE-149 (GNE149) is a potent, full estrogen receptor alpha (ERα) antagonist and degrader with IC50 of 0.053 nM (MCF7, ERα degradation).
GNE-149 exhibits IC50 value of 0.66 nM and 0.69 nM in MCF-7 and T47D proliferation assays.
GNE-149 (0.3-30 mg/kg) showed dose-dependent efficacy in MCF7 xenograft mouse model harboring either wild-type (WT) ERα or overexpressed Y537S mutant

物理化学性质&存储条件

分子量 503.59
分子式 C28H33F4N3O
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

C[C@@H]1CC2=C([C@@H](C3=C(F)C=C(OC4CN(CCCF)C4)C=C3F)N1CC(C)(F)C)NC5=C2C=CC=C5

参考文献

1. Liang J, et al. ACS Med Chem Lett. 2020 May 26;11(6):1342-1347.

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