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1443752-76-8

1443752-76-8 structure
1443752-76-8 structure
  • Name: OP-1074
  • Chemical Name: OP-1074
  • CAS Number: 1443752-76-8
  • Molecular Formula: C29H31NO4
  • Molecular Weight: 457.56
  • Catalog: Research Areas Cancer
  • Create Date: 2020-01-24 07:58:51
  • Modify Date: 2024-01-10 10:57:07
  • 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].

Name OP-1074
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.

Molecular Formula C29H31NO4
Molecular Weight 457.56