Estrogen receptor α antagonist 1

Names

[ CAS No. ]:
2580941-45-1

[ Name ]:
Estrogen receptor α antagonist 1

Biological Activity

[Description]:

Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 (compound 35) can be used for the research of cancer[1].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Cancer

[Target]

IC50: 0.02 μM (Estrogen receptor α), 6.55 μM (Estrogen receptor β) and 7.73 μM (MCF-7 cells)[1]


[In Vitro]

Estrogen receptor α antagonist 1 (compound 35) (1 nM-100 μM; 72 h)selectively inhibites estrogen receptor α, estrogen receptor β and MCF-7 cells[1]. Cell Viability Assay[1] Cell Line: MCF-7 cells Concentration: 1 nM-100 μM Incubation Time: 72 hours Result: Exhibited IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively at 72 hours.

[References]

[1]. Carr M, et al. Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening. Bioorg Med Chem. 2020 Mar 1;28(5):115261.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H32N2O5

[ Molecular Weight ]:
452.54


Related Compounds