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Giredestrant tartrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Giredestrant tartrate图片
CAS NO:2407529-33-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
GDC-9545 tartrate
产品介绍
Giredestrant tartrate (GDC-9545 tartrate),一种非甾体 ER 配体,也是一种口服有效的,选择性雌激素受体(ER)拮抗剂。Giredestrant tartrate 可以在 ER 配体结合域内与雌二醇竞争结合并诱导构象变化。Giredestrant tartrate 具有抗肿瘤活性。
生物活性

Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selectiveestrogen receptor(ER)antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity[1].

IC50& Target[1]

Estrogen receptor

 

体外研究
(In Vitro)

Giredestrant (GDC-9545) tartrate consistently induces ER turnover and drives deep transcriptional suppression of ER, resulting in robust in vitro anti-proliferative activity[1].

体内研究
(In Vivo)

Giredestrant (GDC-9545) tartrate is an ER antagonist that combines desirable mechanistic and pre-clinical DMPK attributes. The highly potent in vivo efficacy of Giredestrant likely arises due to the particular combination of high binding potency, full suppression of ER signaling, and an improved DMPK profile[1].

Clinical Trial
分子量

672.64

Formula

C31H37F5N4O7

CAS 号

2407529-33-1

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.