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GDC-9545

Chemical Structure : GDC-9545

CAS No.: 1953133-47-5

GDC-9545 (Giredestrant, GDC9545, RG6171)

Catalog No.: PC-72786Not For Human Use, Lab Use Only.

GDC-9545 (Giredestrant) is an efficient and potent selective estrogen receptor degrader (SERD) and a full antagonist.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GDC-9545 (Giredestrant) is an efficient and potent selective estrogen receptor degrader (SERD) and a full antagonist.
GDC-9545 exhibited better antiproliferation activity than known SERDs across multiple cell lines.
GDC-9545 exhibits low drug-drug interaction liability and demonstrates excellent in vitro and in vivo safety profiles.
GDC-9545 induced tumor regressions either as a single agent or in combination with a CDK4/6 inhibitor in an ESR1Y537S mutant PDX or a wild-type ERα tumor model.

Physicochemical Properties

M.Wt 522.564
Formula C27H31F5N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO (5.2 mg/mL)

Chemical Name/SMILES

3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol

References

1. Liang J, et al. J Med Chem. 2021 Aug 26;64(16):11841-11856.

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