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LSZ102

Chemical Structure : LSZ102

CAS No.: 2135600-76-7

LSZ102 (LSZ 102;LSZ-102)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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).

Physicochemical Properties

M.Wt 470.462
Formula C25H17F3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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

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