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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Estrogen Receptor/ERR-LSZ102
LSZ102

Chemical Structure : LSZ102

CAS No.: 2135600-76-7

LSZ102 (LSZ 102;LSZ-102)

货号: PC-63293Not For Human Use, Lab Use Only.

LSZ102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with ERα transcription IC50 of 6 nM and ERα degradation IC50 of 0.2 nM.

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5 mg ¥2280 In stock
25 mg ¥5280 In stock
100 mg ¥12800 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LSZ102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with ERα transcription IC50 of 6 nM and ERα degradation IC50 of 0.2 nM.
LSZ102 robustly causes inhibition of cell proliferation in MCF-7 cells with IC50 of 1.7 nM, inhibits the mRNA level of canonical endogenous ER target gene GREB1 with IC50 of 8.9 nM.
LSZ102 demonstrates anti-tumor efficacy in the ER+ human breast cancer MCF-7 xenograft model (10 mg/kg).

物理化学性质&存储条件

分子量 470.462
分子式 C25H17F3O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-3-(4-((2-(2-(1,1-Difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic acid

参考文献

1. Tria GS, et al. J Med Chem. 2018 Apr 12;61(7):2837-2864.

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