LSZ102 |
| Catalog No.GC18155 |
LSZ102 es un potente degradador selectivo del receptor de estrógeno biodisponible por vía oral con una IC50 de 0,2 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2135600-76-7
Sample solution is provided at 25 µL, 10mM.
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LSZ102 exhibit oral bioavailability and preclinical activity as selective estrogen receptor degraders (SERDs). It is a compound in clinical development for the treatment of ERα positive breast cancer.
In Phase I/Ib trials for the treatment of ERα positive breast cancer, LSZ-102 has an IC50 of 0.2 nM. LSZ-102 induces significant degradation of ERα after 24 h, when given as a 10 μM solution to MCF-7 cells.
Treatment of the mice with LSZ102 once daily at 20 mg/kg resulted in significant tumor growth inhibition as compared to the control group treated with vehicle alone, resulting in tumor stasis (mean change in tumor volume of LSZ102 vs control = %ΔT/ΔC of 2.4% on day 48, p < 0.05).
Dosing of 3 mg/kg solution of LSZ102 in male Sprague−Dawley rats resulted in 33% bioavailability and a dose-normalized exposure of 620 nM·h
References
1. Tria GS, et al. Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. J Med Chem. 2018 Apr 12;61(7):2837-2864.
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