ERβ-targeted NIR probe P5
ERβ-targeted NIR probe P5 is an ERβ-selective fluorescent probe that binds preferentially to ERβ over ERα, enabling near-infrared fluorescence imaging of ERβ in living cells and in vivo. ERβ-targeted NIR probe P5 supports measurement of ERβ diffusion coefficient via fluorescence recovery after photobleaching. ERβ-targeted NIR probe P5 shows low cytotoxicity across multiple cell types, preserves ERβ expression, accumulates at ERβ-overexpressing tumor sites in vivo, and exhibits minimal fluorescence fluctuation across varied pH and cellular analyte conditions. ERβ-targeted NIR probe P5 can be used for the research of prostate cancer.
For research use only. We do not sell to patients.
- CAS No.: 2890606-81-0
- Formula: C20H12N2O3
- Molecular Weight:328.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ERβ |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
>100 μM
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Cytotoxicity against human MCF-10A normal breast cells assessed by MTT cell viability assay after 72 h incubation.
Cytotoxicity against human MCF-10A normal breast cells assessed by MTT cell viability assay after 72 h incubation.
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34914372 |
| MCF7 | IC50 |
>100 μM
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Cytotoxicity against human MCF-7 breast cancer cells assessed by MTT cell viability assay after 72 h incubation.
Cytotoxicity against human MCF-7 breast cancer cells assessed by MTT cell viability assay after 72 h incubation.
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34914372 |
| DU-145 | IC50 |
79.16 μM
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Cytotoxicity against human DU-145 prostate cancer cells assessed by MTT cell viability assay after 72 h incubation.
Cytotoxicity against human DU-145 prostate cancer cells assessed by MTT cell viability assay after 72 h incubation.
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34914372 |
In Vitro
ERβ-targeted NIR probe P5 binds selectively to ERβ LBD with an RBA of 4.612 and 6.579-fold selectivity over ERα[1].
ERβ-targeted NIR probe P5 exhibits NIR emission, a large Stokes shift, linear fluorescence response in the 1-100 μM range, and strong anti-interference stability against pH, cellular analytes, and ionic strength[1].
ERβ-targeted NIR probe P5 (Compound P5) (72h) exhibits low cytotoxicity in MCF-10A, MCF-7, and DU-145 cells, with IC50 values of >100, >100, and 79.16 μM, respectively[1].
ERβ-targeted NIR probe P5 (10 μM; 30 min) selectively labels ERβ in DU-145 prostate cancer cells, localizes to both nucleus and cytoplasm, and shows high colocalization with ERβ antibody staining[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 breast cancer cells, DU-145 prostate cancer cells
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Concentration:10 μM (P5); 100 μM (estradiol, competitive co-incubation)
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Incubation Time:30 min (P5 incubation); 30 min (competitive co-incubation with estradiol); 10 min (Hoechst 33342 staining); 30 min (Mito-tracker Green staining); 12 h (anti-ERβ primary antibody incubation); 1 h (DyLight 488 secondary antibody incubation)
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Result:Emitted strong fluorescence in ERβ-overexpressing DU-145 cells but very weak fluorescence in ERα-overexpressing MCF-7 cells.
Showed no obvious fluorescence when excess estradiol was co-administered.
Distributed in both the nucleus and cytoplasm of DU-145 cells and showed strong ERβ labeling with a high colocalization rate with ERβ immunofluorescence staining.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (male; 6 weeks old)[1]
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Dosage:0.4 μg/kg
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Administration:i.v.; single dose
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Result:Reached maximum tumor fluorescence intensity at 18 h post-injection.
Tumor fluorescence disappeared from the tumor site 28 h after injection.
Chemical Information
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CAS No. 2890606-81-0
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Molecular Weight 328.32
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Formula C20H12N2O3
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SMILES
N#C/C(C#N)=C(C1=CC(O)=CC=C1O2)\C=C2/C=C/C3=CC=C(O)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ERβ-targeted NIR probe P5 Related Classifications
HY-D3614 Related Classifications
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