Giredestrant 是一种口服有效的、选择性的、非甾体的雌激素受体 (ER) 拮抗剂，具有抗肿瘤作用。它可以在 ER 配体结合域内与雌二醇 (Estradiol) 竞争结合并诱导构象变化。

Giredestrant potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity. Giredestrant, a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist.

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.Giredestrant (GDC-9545) is a novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes.

1953133-47-5

C27H31F5N4O

522.55

GDC-9545

DMSO:100mg/mL (191.37 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years