LSZ-102是一种有效和选择性的雌激素受体降解剂（IC50 = 0.2 nM），可用于有关ERα阳性乳腺癌的研究。

LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer.

LSZ-102 causes significant degradation of ERα after 24 h when given as a 10 μM solution to MCF-7 cells. LSZ-102 currently in Phase I/Ib trials for the treatment of ERα positive breast cancer. 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 show that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 (IC50: 0.3 nM)[1].

In male Sprague-Dawley rats, LSZ-102 (3 mg/kg) causes 33% bioavailability and a dose-normalized exposure of 620 nMoh. In mice, LSZ-102 (20 mg/kg) causes significant tumor growth inhibition resulting in tumor stasis[1].

2135600-76-7

C25H17F3O4S

470.46

LSZ-102

DMSO:100 mg/mL (212.56 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years