NSC23925 (free base)

NSC23925 (free base) is a novel, selective and effective P-glycoprotein (Pgp) inhibitor. IC50 & Target: P-glycoprotein^[1] In Vitro: SKOV-3 cells with long-term exposure of 1 μM NSC23925 (free base) (SKOV-3/NSC23925 (free base)) shows stable growth in culture medium. NSC23925 (free base) specifically inhibits Pgp overexpression to prevent the emergence of paclitaxel resistance during paclitaxel treatment^[1]. NSC23925 (free base) 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 (free base) doses between 0.5 and 1 µM. the presence of < 5 to 10 µM of NSC23925 (free base) alone has no cytotoxic effect in the parental cell lines SKOV-3 and OVCAR8 which lack expression of Pgp1. he IC₅₀ for NSC23925 (free base) is 8 µM in SKOV-3/SKOV-3_TR and 25 µM in OVCAR8/OVCAR8_TR cell lines, whereas the mean concentration of NSC23925 (free base) required for maximal reversal of resistance in SKOV-3_TR or OVCAR8_TR to cytotoxic drugs is 0.5 µM to 1 µM^[2]. In Vivo: Both saline alone and NSC23925 (free base) alone treated tumors grow progressively. The usage of NSC23925 (free base) in paclitaxel chemotherapy produces significantly prolongs anticancer efficacy of paclitaxel^[1].