NSC 23925B

NSC 23925B is a P-glycoprotein (P-gp) inhibitor, as well as the most biologically active isomer of NSC23925 (HY-19626), which reverses and prevents P-glycoprotein-mediated multidrug resistance in cancer cells. NSC 23925B shows weak inhibition against most CYP450 enzymes (IC₅₀ > 10 μM), and exhibits moderate inhibitory activity against CYP2B6 and CYP2D6 with IC₅₀ values of 8.589 μM and 1.407 μM, respectively. NSC 23925B can be used for the research of multidrug-resistant cancers^[1]. In Vitro:NSC 23925B potently reverses Pgp-mediated multidrug resistance (MDR) in multidrug-resistant human breast cancer and colon cancer cell lines^[1].
NSC 23925B inhibits Pgp-mediated chemoresistance in ovarian cancer cells and osteosarcoma cells^[1]. In Vivo:NSC 23925B (2.50-93.75 mg/kg; i.p.; i.v.; single dose) exhibits favorable pharmacokinetic profiles with high bioavailability, measurable plasma concentrations over 24 hours, and limited toxicity in male BALB/c mice, with a maximum tolerated dose of at least 68.80 mg/kg (i.p.) in males and 24.70 mg/kg (i.v.) in both sexes^[1].
NSC 23925B (2.50-47.20 mg/kg; i.p.; i.v.; single dose) exhibits favorable pharmacokinetic profiles with high bioavailability, measurable plasma concentrations over 24 hours, and limited toxicity in male Sprague-Dawley rats, with a maximum tolerated dose of at least 33.10 mg/kg (i.p.) and 38.80 mg/kg (i.v.) in males^[1].