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].

Product Specifications

CAS Number

[2407529-33-1]

Product Name Alternative

GDC-9545 (tartrate) ; RG6171 (tartrate)

UNSPSC

12352005

Target

Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/estrogen-receptor-antagonist-1.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C31H37F5N4O7

Molecular Weight

672.64

References & Citations

[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.