GNE-149

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GNE-149 

GNE-149 是一种有效的，具有口服活性的雌激素受体 α (ERα; IC50=0.053 nM) 拮抗剂。GNE-149 也是一种选择性的雌激素受体降解剂 (SERD)。GNE-149 可用于乳腺癌的研究。

GNE-149

GNE-149 Chemical Structure

CAS No. : 1953132-75-6

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生物活性

GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer[1].

IC50 & Target[1]

ERα

0.053 nM (IC50)

体外研究
(In Vitro)

GNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC50s of 0.66 and 0.69 nM, respectively[1].
GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC50s of 0.053 and 0.031 nM, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

GNE-149 (0.3-30 mg/kg) exhibits in vivo efficacy in an MCF7 xenograft mouse model harboring either wild-type (WT) ERα or overexpressed Y537S mutant[1].
GNE-149 has favorable pharmacokinetic profile, including total clearance (CL; 19, 8, and 13 mL/min/kg for Rat, Dog, and Cyno) and oral bioavailability (F; 31%, 49%, and 28% for Rat, Dog, and Cyno)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Crl:NU Foxn1 nu mice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor[1]
Dosage: 0.3, 1, 3, 10, and 30 mg/kg
Administration: Orally q.d. for 21 days
Result: Exhibited dose-dependent efficacy in the MCF7 WT and Y537S mutant xenograft model, with tumor regression observed at all doses above 0.3 mg/kg in Y537S mutant xenograft model.

分子量

503.57

Formula

C28H33F4N3O
CAS 号

1953132-75-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Jun Liang, et al. Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer. ACS Med Chem Lett. 2020 May 26;11(6):1342-1347.

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