Giredestrant tartrate(Synonyms: GDC-9545 tartrate)

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Giredestrant tartrate (Synonyms: GDC-9545 tartrate)

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。

Giredestrant tartrate(Synonyms: GDC-9545 tartrate)

Giredestrant tartrate Chemical Structure

CAS No. : 2407529-33-1

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Giredestrant tartrate 的其他形式现货产品:

Giredestrant

生物活性

Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen 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].

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)

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].

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

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.

参考文献
  • [1]. C Metcalfe, et al. Abstract P5-04-07: GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes.

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