Brilanestrant (GDC-0810)

Product Specifications

CAS Number

1365888-06-7

Synonyms

ARN-810

Target

Estrogen/progestogen Receptor

Applications

Endocrinology & Hormones

Smiles

CCC (=C (C1=CC=C (C=C1) C=CC (=O) O) C2=CC3=C (C=C2) NN=C3) C4=C (C=C (C=C4) F) Cl

Molecular Formula

C26H20ClFN2O2

Additionnal Information

Brilanestrant (GDC-0810, ARN-810) is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors.