2407529-33-1
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
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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 |
| Molecular Formula | C31H37F5N4O7 |
|---|---|
| Molecular Weight | 672.64 |