OP-1074

Modify Date: 2025-08-25 19:20:03

OP-1074 Structure
OP-1074 structure
Common Name OP-1074
CAS Number 1443752-76-8 Molecular Weight 457.56
Density N/A Boiling Point N/A
Molecular Formula C29H31NO4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name OP-1074

 OP-1074 Biological Activity

Description 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].
Related Catalog
Target

ERα

ERβ

In Vitro 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.
References

[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.

 Chemical & Physical Properties

Molecular Formula C29H31NO4
Molecular Weight 457.56
InChIKey KDVXAPCZVZMPMU-XBBWARJSSA-N
SMILES CC1=C(c2ccc(O)cc2)C(c2ccc(OCCN3CCC(C)C3)cc2)Oc2cc(O)ccc21
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