Hapalosin

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.