Giredestrant

1953133-47-5

522.55

H2O : < 0.1 mg/mL (insoluble); DMSO : 100 mg/mL (191.37 mM; Need ultrasonic)

Others

Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity^[1]. In Vitro: Giredestrant (GDC-9545) is a novel 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].