OP-1074

OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively[1].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

ERα

ERβ

OP-1074 (0-100 nM; 24 hours) inhibits  MCF-7 cells  and CAMA-1 cells proliferation with IC50 values of 6.3 and 9.2 nM, respectively[1]. OP-1074 (100 nM; 24 hours) destabilizatizes ERα protein expression in MCF-7 and CAMA-1 cells[1]. Cell Viability Assay[1] Cell Line: MCF-7 cells, CAMA-1 cells Concentration: 0 nM, 10 nM,100 nM Incubation Time: 24 hours Result: Inhibited breast cancer cell proliferation. Western Blot Analysis[1] Cell Line: MCF-7 cells, CAMA-1 cells Concentration: 100 nM Incubation Time: 24 hours Result: Downregulated ERα protein expression.

[1]. Fanning SW, et al. Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.Nat Commun. 2018 Jun 18;9(1):2368.