1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. 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.

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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5 mg USD 850 In-stock
10 mg USD 1450 In-stock
25 mg USD 2950 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (218.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1855 mL 10.9275 mL 21.8551 mL
5 mM 0.4371 mL 2.1855 mL 4.3710 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1855 mL 10.9275 mL 21.8551 mL 54.6376 mL
5 mM 0.4371 mL 2.1855 mL 4.3710 mL 10.9275 mL
10 mM 0.2186 mL 1.0928 mL 2.1855 mL 5.4638 mL
15 mM 0.1457 mL 0.7285 mL 1.4570 mL 3.6425 mL
20 mM 0.1093 mL 0.5464 mL 1.0928 mL 2.7319 mL
25 mM 0.0874 mL 0.4371 mL 0.8742 mL 2.1855 mL
30 mM 0.0729 mL 0.3643 mL 0.7285 mL 1.8213 mL
40 mM 0.0546 mL 0.2732 mL 0.5464 mL 1.3659 mL
50 mM 0.0437 mL 0.2186 mL 0.4371 mL 1.0928 mL
60 mM 0.0364 mL 0.1821 mL 0.3643 mL 0.9106 mL
80 mM 0.0273 mL 0.1366 mL 0.2732 mL 0.6830 mL
100 mM 0.0219 mL 0.1093 mL 0.2186 mL 0.5464 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
OP-1074
Cat. No.:
HY-125263
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