BCRP-IN-1
BCRP-IN-1 (compound 48) is a potent inhibitor of breast cancer resistance protein (BCRP), with IC50s of 2.92 μM and 2.46 μM in Hoechst 33342 assay and Pheophorbide A assay, respectively.
For research use only. We do not sell to patients.
- CAS No.: 765899-28-3
- Formula: C16H14N4O4
- Molecular Weight:326.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MDCK-II | IC50 |
2.46 μM
Compound: 48
|
Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up to 120 mins by flow cytometry
Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up to 120 mins by flow cytometry
|
[PMID: 24184213] |
| MDCK-II | IC50 |
2.92 μM
Compound: 48
|
Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay
Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay
|
[PMID: 24184213] |
Chemical Information
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CAS No. 765899-28-3
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Molecular Weight 326.31
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Formula C16H14N4O4
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SMILES
O=[N+](C1=CC=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1)[O-]
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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.
Protocols
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Nuclear DNA counterstaining and nuclear morphology staining
Nuclear DNA counterstaining uses DNA-binding fluorescent dyes to visualize nuclei and chromatin so that nuclei can be located, counted, segmented, and evaluated for morphology; Hoechst 33342, DAPI, propidium iodide, and DRAQ5 are commonly reported nuclear stains, while live-cell DNA labeling is better supported for Hoechst dyes and DRAQ5 than for propidium iodide in intact viable cells. Nuclear morphology staining can detect apoptosis-associated nuclear changes, including chromatin condensation, nuclear shrinkage, nuclear fragmentation, reduced nuclear area/perimeter/axis length, and increased nuclear fluorescence intensity; these morphology readouts have been compared with apoptosis markers such as TUNEL and caspase-3 immunofluorescence.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)