P-gp modulator-6
P-gp modulator-6 is a P-glycoprotein (P-gp) modulator. P-gp modulator-6 regulates the substrate specificity of P-gp and enhances the efflux activity of Daunorubicin (HY-13062A) and Rhodamine 123 (HY-D0816). P-gp modulator-6 can be used in the research of multidrug-resistant cancers. P-gp modulator-6 can be used in the research of multidrug-resistant pancreatic cancer and multidrug-resistant colon cancer.
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- No. CAS: 352652-36-9
- Fòrmula: C16H13ClN2O2
- Peso molecular:300.74
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
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P-gp |
P-gp modulator-6 (10 μM; 2 h) more potently stimulates P-gp-mediated efflux of daunorubicin than Rho-123 in mouse fibroblast Con A cells when used at 10 μM for 2 h[1].
P-gp modulator-6 (Dilution series; 5 days) exhibits similar antiproliferative activity against parental EPG85-257P and daunorubicin-resistant EPG85-257RDB gastric carcinoma cells, with reduced activity against mitoxantrone-resistant EPG85-257RNOV gastric carcinoma cells (IC50 = 53.8 µM, RR = 2.51)[2].
P-gp modulator-6 (Dilution series; 5 days) exhibits antiproliferative activity against parental EPP85-181P pancreatic carcinoma cells, with reduced activity against daunorubicin-resistant EPP85-181RDB cells and increased activity against mitoxantrone-resistant EPP85-181RNOV cells (IC50 = 33.6 µM, RR = 0.61)[2].
P-gp modulator-6 (Dilution series; 5 days) exhibits antiproliferative activity against parental HT-29P colon carcinoma cells, with a collateral sensitivity effect against daunorubicin-resistant HT-29RDB cells (IC50 = 30.7 µM, RR = 0.50) and mitoxantrone-resistant HT-29RNOV cells (IC50 = 19.3 µM, RR = 0.31)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human gastric carcinoma cell lines (parental EPG85-257P, daunorubicin-resistant EPG85-257RDB, mitoxantrone-resistant EPG85-257RNOV)
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Concentration:Dilution series
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Incubation Time:5 days
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Result:Exhibited antiproliferative activity against parental EPG85-257P cells with an IC50 of 21.4 µM.
Showed similar antiproliferative activity against daunorubicin-resistant EPG85-257RDB cells with an IC50 of 19.9 µM and a relative resistance ratio (RR) of 0.93.
Had reduced antiproliferative activity against mitoxantrone-resistant EPG85-257RNOV cells with an IC50 of 53.8 µM and an RR of 2.51.
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Cell Line:Human pancreatic carcinoma cell lines (parental EPP85-181P, daunorubicin-resistant EPP85-181RDB, mitoxantrone-resistant EPP85-181RNOV)
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Concentration:Dilution series
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Incubation Time:5 days
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Result:Exhibited antiproliferative activity against parental EPP85-181P cells with an IC50 of 55.1 µM.
Had reduced antiproliferative activity against daunorubicin-resistant EPP85-181RDB cells with an IC50 of 85.6 µM and an RR of 1.55.
Showed increased antiproliferative activity against mitoxantrone-resistant EPP85-181RNOV cells with an IC50 of 33.6 µM and an RR of 0.61.
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Cell Line:human colon carcinoma cell lines (parental HT-29P, daunorubicin-resistant HT-29RDB, mitoxantrone-resistant HT-29RNOV)
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Concentration:Dilution series
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Incubation Time:5 days
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Result:Exhibited antiproliferative activity against parental HT-29P cells with an IC50 of 61.5 µM.
Showed increased antiproliferative activity against daunorubicin-resistant HT-29RDB cells with an IC50 of 30.7 µM and an RR of 0.50.
Showed increased antiproliferative activity against mitoxantrone-resistant HT-29RNOV cells with an IC50 of 19.3 µM and an RR of 0.31.
Chemical Information
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No. CAS 352652-36-9
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Peso molecular 300.74
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Fòrmula C16H13ClN2O2
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SMILES
ClC1=CC=C(CC2=NOC(C3=C(OC)C=CC=C3)=N2)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Kondratov RV, et al. Small molecules that dramatically alter multidrug resistance phenotype by modulating the substrate specificity of P-glycoprotein. Proceedings of the National Academy of Sciences of the United States of America. 2001 Nov 20;98(24):14078-83. [Content Brief]
[2]. Ramalhete C, et al. Triterpenoids from Momordica balsamina with a Collateral Sensitivity Effect for Tackling Multidrug Resistance in Cancer Cells. Planta medica. 2018 Dec;84(18):1372-1379. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
P-gp modulator-6 Related Classifications
HY-164585 Related Classifications
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- P-gp modulator-6
- 352652-36-9
- P-glycoprotein
- mouse fibroblast Con A cells
- EPG85-257P gastric carcinoma cells
- multidrug-resistant pancreatic carcinoma
- multidrug-resistant colon carcinoma
- daunorubicin
- EPG85-257RDB gastric carcinoma cells
- multidrug-resistant cancer
- Rhodamine 123
- HT-29P colon carcinoma cells
- Inhibitor
- inhibitor
- inhibit