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  3. OP-1074

OP-1074 

Cat. No.: HY-125263
Handling Instructions

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.

For research use only. We do not sell to patients.

OP-1074 Chemical Structure

OP-1074 Chemical Structure

CAS No. : 1443752-76-8

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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].

IC50 & Target[1]

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.
Molecular Weight

457.56

Formula

C₂₉H₃₁NO₄

CAS No.

1443752-76-8

SMILES

OC1=CC2=C(C=C1)C(C)=C(C3=CC=C(O)C=C3)[[email protected]](C4=CC=C(OCCN5CC[[email protected]@H](C)C5)C=C4)O2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

OP-1074OP1074OP 1074Estrogen Receptor/ERRantiestrogen,ERαERβInhibitorinhibitorinhibit

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