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2407529-33-1

2407529-33-1 structure
2407529-33-1 structure
  • Name: Giredestrant tartrate
  • Chemical Name: Giredestrant tartrate
  • CAS Number: 2407529-33-1
  • Molecular Formula: C31H37F5N4O7
  • Molecular Weight: 672.64
  • Catalog: Signaling Pathways Others Estrogen Receptor/ERR
  • Create Date: 2020-06-01 18:54:46
  • Modify Date: 2024-01-22 07:56:00
  • 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].

Name Giredestrant tartrate
Description 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].
Related Catalog
Target

Estrogen receptor

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].
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].
References

[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.

Molecular Formula C31H37F5N4O7
Molecular Weight 672.64