Hapalosin
Hapalosin is a multidrug resistance reversal agent and chemosensitizer with mild cytotoxicity against cancer cells. Hapalosin inhibits the ATP-dependent drug efflux pump function of P-glycoprotein and antagonizes multidrug resistance-associated proteins. Hapalosin reverses multidrug resistance mediated by P-glycoprotein and multidrug resistance-associated proteins, increases the intracellular accumulation of drugs transported by P-glycoprotein, and enhances the cytotoxicity of these drugs against cancer cells overexpressing P-glycoprotein. Hapalosin can be used in the research of multidrug-resistant cancers.
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- No. CAS: 159542-04-8
- Fòrmula: C28H43NO6
- Peso molecular:489.64
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
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| HL-60 | EC50 |
0.7 μg/mL
Compound: hapalosin
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Effective concentration against HL-60/ADR cells using MRP-mediated MDR assay using 2 nM vincristine which results in 50% of the cells being killed in the presence of particular cytotoxic drug.
Effective concentration against HL-60/ADR cells using MRP-mediated MDR assay using 2 nM vincristine which results in 50% of the cells being killed in the presence of particular cytotoxic drug.
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[PMID: 9526572] |
Hapalosin (1-6 µg/mL; 48 h) reverses P-gp-mediated multidrug resistance (MDR) in MCF-7/ADR cells, with an EC50 of 1 µg/mL; meanwhile, the compound has an IC20 of 6 µg/mL for intrinsic cytotoxicity against these cells[1].
Hapalosin (0.7-6 µg/mL; 48 h) reverses MRP-mediated multidrug resistance (MDR) in HL-60/ADR cells, with an EC50 of 0.7 µg/mL; meanwhile, the IC20 for its intrinsic cytotoxicity against these cells is 6 µg/mL[1].
Hapalosin (60 min) effectively increases the intracellular accumulation of [3H]-Vinblastine (HY-13780) in MCF-7/ADR cells, indicating that it inhibits P-gp-mediated drug efflux[1].
Hapalosin (20 μM; 90 min) increases the accumulation of [3H]-Vinblastine and [3H]-Paclitaxel (HY-B0015) in SKVLB1 cells by inhibiting the P-glycoprotein efflux pump; at a concentration of 20 μM, the accumulation of [3H]-Paclitaxel increases by 440% compared with the control group, while this compound does not affect drug accumulation in SKOV3 cells[2].
Hapalosin (2.5-12.5 μM; 48 h) selectively enhances the cytotoxicity of chemotherapeutic drugs transported by P-glycoprotein against MCF-7/ADR cells at concentrations ≥ 2.5 μM, and completely reverses P-glycoprotein-mediated multidrug resistance to vinblastine in these cells at a concentration of 5 μM[2].
Hapalosin exhibits cytotoxicity against KB, LoVo and MCF-7/ADR cells, with IC50 values of 2.5 μg/mL, 2 μg/mL and 5-15 μM[2], respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7/ADR (P-gp-overexpressing, MRP-negative breast carcinoma cells)
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Concentration:6 µg/mL (alone); 1 µg/mL (in presence of 25 nM actinomycin D)
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Incubation Time:48 h
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Result:Exhibited an IC20 of 6 µg/mL for intrinsic cytotoxicity.
Exhibited an EC50 of 1 µg/mL for reversing P-gp-mediated MDR in the presence of actinomycin D.
Was more effective at reversing P-gp-mediated MDR than all tested D-glucose mimetics of hapalosin.
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Cell Line:HL-60/ADR (MRP-expressing, P-gp-negative promyelocytic leukemia cells)
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Concentration:6 µg/mL (alone); 0.7 µg/mL (in presence of 2 nM vincristine)
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Incubation Time:48 h
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Result:Exhibited an IC20 of 6 µg/mL for intrinsic cytotoxicity.
Exhibited an EC50 of 0.7 µg/mL for reversing MRP-mediated MDR in the presence of vincristine.
Showed similar efficacy in reversing MRP-mediated MDR to select D-glucose mimetics.
Chemical Information
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No. CAS 159542-04-8
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Peso molecular 489.64
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Fòrmula C28H43NO6
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SMILES
CN(C([C@@H](OC([C@H]([C@H](OC(C[C@H]1O)=O)CCCCCCC)C)=O)C(C)C)=O)[C@H]1CC2=CC=CC=C2
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hapalosin Related Classifications
HY-182633 Related Classifications
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