Giredestrant,2407529-33-1

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Giredestrant tartrate

CAS No. : 2407529-33-1

MCE 国际站：Giredestrant tartrate

产品活性：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。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Estrogen Receptor/ERR

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.

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.

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