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

Chemical Structure : Giredestrant

CAS No.: 1953133-47-5

Giredestrant (GDC-9545, GDC9545, RG6171)

货号: PC-72786Not For Human Use, Lab Use Only.

GDC-9545 (Giredestrant) is an efficient and potent selective estrogen receptor degrader (SERD) and a full antagonist.

规格 价格 库存 数量
5 mg ¥1780 In stock
10 mg ¥2780 In stock
25 mg ¥4580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GDC-9545 (Giredestrant) is an efficient and potent selective estrogen receptor degrader (SERD) and a full antagonist.
GDC-9545 exhibited better antiproliferation activity than known SERDs across multiple cell lines.
GDC-9545 exhibits low drug-drug interaction liability and demonstrates excellent in vitro and in vivo safety profiles.
GDC-9545 induced tumor regressions either as a single agent or in combination with a CDK4/6 inhibitor in an ESR1Y537S mutant PDX or a wild-type ERα tumor model.

物理化学性质&存储条件

分子量 522.564
分子式 C27H31F5N4O
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 (5.2 mg/mL)

Chemical Name/SMILES

3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol

参考文献

1. Liang J, et al. J Med Chem. 2021 Aug 26;64(16):11841-11856.

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