Giredestrant tartrate

Modify Date: 2024-01-22 07:56:00

Giredestrant tartrate Structure
Giredestrant tartrate structure
Common Name Giredestrant tartrate
CAS Number 2407529-33-1 Molecular Weight 672.64
Density N/A Boiling Point N/A
Molecular Formula C31H37F5N4O7 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Giredestrant tartrate


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].

 Names

Name Giredestrant tartrate

 Giredestrant tartrate Biological Activity

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.

 Chemical & Physical Properties

Molecular Formula C31H37F5N4O7
Molecular Weight 672.64