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.
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- CAS No.: 7555-80-8
- Formule: C20H20O7
- Masse moléculaire:372.37
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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Cell Line
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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] |
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.
Chemical Information
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CAS No. 7555-80-8
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Masse moléculaire 372.37
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)