2-(P-METHOXYPHENYL)-Α-2-PIPERIDYL-4-QUINOLINEMETHANOL DIHYDROCHLORIDE

P-glycoprotein

NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor. SKOV-3 cells with long-term exposure of 1 μM NSC23925 show stable growth in culture medium. NSC23925 specifically inhibits Pgp overexpression to prevent the emergence of paclitaxel resistance during paclitaxel treatment. NSC23925 reverses chemoresistance in a wide variety of tumor types where Multidrug resistance 1 (MDR1) is highly expressed. Maximal reversal of MDR is typically seen in NSC23925 doses between 0.5 and 1 µM. The IC ₅₀ for NSC23925 is 8 µM in SKOV-3/SKOV-3 _TR and 25 µM in OVCAR8/OVCAR8 _TR cell lines, whereas the mean concentration of NSC23925 required for maximal reversal of resistance in SKOV-3 _TR or OVCAR8 _TR to cytotoxic drugs is 0.5 µM to 1 µM.

Both saline alone and NSC23925 alone treated tumors grow progressively. The usage of NSC23925 in paclitaxel chemotherapy significantly prolongs anticancer efficacy of paclitaxel.