LSZ-102

2135600-76-7

C25H17F3O4S

H2O : < 0.1 mg/mL (insoluble); DMSO : 100 mg/mL (212.56 mM; Need ultrasonic)

Others

LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC₅₀ of 0.2 nM. IC50 & Target: estrogen receptor^[1] In Vitro: LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC₅₀ of 0.2 nM and currently in Phase I/Ib trials for the treatment of ERalpha positive breast cancer. LSZ-102 induces significant degradation of ERalpha after 24 h, when given as a 10 uM solution to MCF-7 cells. Robust inhibition of cell proliferation in MCF-7 cells is observed upon incubation with LSZ-102 with a half inhibitory concentration of 1.7 nM. Results demonstrate that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 with IC₅₀ of 0.3 nM^[1]. In Vivo: Treatment of the mice with LSZ-102 once daily at 20 mg/kg results in significant tumor growth inhibition as compare to the control group treated with vehicle alone, resulting in tumor stasis (mean change in tumor volume of LSZ-102 vs control=%deltaT/deltaC of 2.4% on day 48, p<0.05). Dosing of 3 mg/kg solution of LSZ-102 in male Sprague-Dawley rats results in 33% bioavailability and a dose-normalized exposure of 620 nM-h^[1].