Description
A selective estrogen receptor covalent antagonist; covalently modifies cysteine 530 in the ligand binding domain of wild-type ERα and ERαY537S; inhibits expression of the ERα target genes GREB1 and TFF1 in MCF-7 cells overexpressing wild-type ERα (IC50s = 2.74 and 1.3 nM, respectively), ERαY537S (IC50s = 29.38 and 19.4 nM, respectively), ERαY537N (IC50s = 8.14 and 6.1 nM, respectively), ERαY537C (IC50s = 12.19 and 9.5 nM, respectively), or ERαD538G (IC50s = 24.87 and 4 nM, respectively); inhibits the growth of MCF-7 cells overexpressing wild-type ERα or ERαY537S (GI50s = 1.3 and 8.3 nM, respectively); reduces tumor growth in an MCF-7 mouse xenograft model and an ERαY537S/WT ST941 PDX mouse model in a dose-dependent manner
Formal name: (2E)-4-[[2-[4-[(1E)-1-(1H-indazol-5-yl)-2-phenyl-1-buten-1-yl]phenoxy]ethyl]amino]-N,N-dimethyl-2-butenamide
Synonyms:
Molecular weight: 494.6
CAS: 2052128-15-9
Purity: ≥98%
Formulation: A crystalline solid
