| Identification | Back Directory | [Name]
Estrogen receptor antagonist 1 | [CAS]
2407529-33-1 | [Synonyms]
Giredestrant tartrate
Estrogen receptor antagonist 1 | [Molecular Formula]
C31H37F5N4O7 | [MDL Number]
MFCD32709982 | [MOL File]
2407529-33-1.mol | [Molecular Weight]
672.65 |
| Hazard Information | Back Directory | [Description]
Giredestrant, also known as GDC-9545 and RG6171, is a SERD. GDC-9545 is an orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD GDC-9545 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation. | [Uses]
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]. | [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]. | [IC 50]
Estrogen receptor | [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. |
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