LSZ102

CAS No. 2135600-76-7

LSZ102( LSZ 102 | LSZ-102 )

Catalog No. M13402 CAS No. 2135600-76-7

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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    LSZ102
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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; 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; demonstrates anti-tumor efficacy in the ER+ human breast cancer MCF-7 xenograft model (10 mg/kg).Breast Cancer Phase 1 Clinical.
  • In Vitro
    LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM and currently in Phase I/Ib trials for the treatment of ERα positive breast cancer. LSZ-102 induces significant degradation of ERα after 24 h, when given as a 10 μM solution to MCF-7 cells. Robust inhibition of cell proliferation in MCF-7 cells is observed upon incubation with LSZ-102 with a half inhibitory concentration of 1.7 nM. Results demonstrate that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 with IC50 of 0.3 nM.
  • In Vivo
    Treatment of the mice with LSZ-102 once daily at 20 mg/kg results in significant tumor growth inhibition as compare to the control group treated with vehicle alone, resulting in tumor stasis (mean change in tumor volume of LSZ-102 vs control=%ΔT/ΔC of 2.4% on day 48, p<0.05). Dosing of 3 mg/kg solution of LSZ-102 in male Sprague-Dawley rats results in 33% bioavailability and a dose-normalized exposure of 620 nM?h.
  • Synonyms
    LSZ 102 | LSZ-102
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    Estrogen Receptor/ERR
  • Research Area
    Cancer
  • Indication
    Breast Cancer

Chemical Information

  • CAS Number
    2135600-76-7
  • Formula Weight
    470.462
  • Molecular Formula
    C25H17F3O4S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 100 mg/mL 212.56 mM; H2O : < 0.1 mg/mL
  • SMILES
    O=C(O)/C=C/C1=CC=C(OC2=C(C3=CC=C(F)C=C3C(F)(F)C)SC4=CC(O)=CC=C42)C=C1
  • Chemical Name
    (E)-3-(4-((2-(2-(1,1-Difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic acid

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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