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  3. Giredestrant tartrate

Giredestrant tartrate (Synonyms: GDC-9545 tartrate)

Cat. No.: HY-135903
Handling Instructions

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.

For research use only. We do not sell to patients.

Giredestrant tartrate Chemical Structure

Giredestrant tartrate Chemical Structure

CAS No. : 2407529-33-1

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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].

IC50 & Target[1]

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].

Molecular Weight

672.64

Formula

C₃₁H₃₇F₅N₄O₇

CAS No.

2407529-33-1

SMILES

C[[email protected]](C1)N(CC(F)(F)CO)[[email protected]](C2=C(F)C=C(NC3CN(CCCF)C3)C=C2F)C4=C1C5=C(N4)C=CC=C5.OC([[email protected]](O)[[email protected]@H](O)C(O)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GiredestrantGDC-9545GDC9545GDC 9545Estrogen Receptor/ERRnon-steroidalERligandorallyconformationalchangeanti-tumoranti-proliferativetranscriptionInhibitorinhibitorinhibit

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Product name:
Giredestrant tartrate
Cat. No.:
HY-135903
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