Pentamethoxymorin
Pentamethoxymorin (MRS923) is a selective breast cancer resistance protein (BCRP/ABCG2) inhibitor. Pentamethoxymorin shows selectivity for BCRP over P-gp and MRP1. Pentamethoxymorin inhibits MDCK BCRP cells with IC50 vaues of 5.98 μM and 5.94 μM in Hoechst 33342 (HY-15559) assay and Pheophorbide A (HY-125665) assay, respectively. Pentamethoxymorin can be used for the study of ccancer.
For research use only. We do not sell to patients.
- CAS No.: 7555-80-8
- Formula: C20H20O7
- Molecular Weight:372.37
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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 |
|---|---|---|---|---|
| A2780 ADR | IC50 |
27.1 μM
Compound: 11
|
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
|
[PMID: 23851114] |
| MDCK-II | IC50 |
5.94 μM
Compound: 11
|
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry
|
[PMID: 23851114] |
| MDCK-II | IC50 |
5.98 μM
Compound: 11
|
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay
Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay
|
[PMID: 23851114] |
In Vitro
Pentamethoxymorin (compound 11) (0.031-100 µM; 30 min-72 h) inhibits BCRP and weakly inhibits P-gp, with no MRP1 inhibition and low cytotoxicity (IC50 = 5.94-5.98 μM for BCRP, 27.1 μM for P-gp)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 7555-80-8
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Molecular Weight 372.37
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Formula C20H20O7
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SMILES
O=C1C(OC)=C(OC2=CC(OC)=CC(OC)=C21)C=3C=CC(OC)=CC3OC
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Synonyms
MRS923
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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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)