Chemical Structure : LSZ102
CAS No.: 2135600-76-7
Catalog No.: 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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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).
M.Wt | 470.462 | |
Formula | C25H17F3O4S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(E)-3-(4-((2-(2-(1,1-Difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic acid |
1. Tria GS, et al. J Med Chem. 2018 Apr 12;61(7):2837-2864.
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