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LSZ102
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
LSZ102图片
CAS NO:2135600-76-7
包装与价格：
包装价格(元)
25mg电议
5mg电议

产品介绍
LSZ102 是一种有效的、口服生物可利用的选择性雌激素受体降解剂，IC50 为 0.2 nM。
Cas No.2135600-76-7
化学名(E)-3-(4-((2-(2-(1,1-difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic
Canonical SMILESOC(/C=C/C1=CC=C(OC2=C(C3=C(C(F)(F)C)C=C(F)C=C3)SC4=C2C=CC(O)=C4)C=C1)=O
分子式C25H17F3O4S
分子量470.46
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

LSZ102

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.