LSZ-102

SKU: orb1308113

Description

LSZ-102 is a potent and selective estrogen receptor degrader with an IC50 of 0.2 nM. It is a valuable research tool for investigating ERα-positive breast cancer in both cellular and animal models, facilitating studies on targeted protein degradation and therapeutic mechanisms.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2135600-76-7
• MW: 470.46
• Purity: 98.56% (May vary between batches)
• Formula: C₂₅H₁₇F₃O₄S
• SMILES: CC(F)(F)c1cc(F)ccc1-c1sc2cc(O)ccc2c1Oc1ccc(\C=C\C(O)=O)cc1
• Target: Estrogen Receptor/ERR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.25 mM);DMSO:90 mg/mL (191.3 mM)

Bioactivity

• In Vivo:
  In male Sprague-Dawley rats, LSZ-102 (3 mg/kg) causes 33% bioavailability and a dose-normalized exposure of 620 nM•h. In mice, LSZ-102 (20 mg/kg) causes significant tumor growth inhibition resulting in tumor stasis.
• In Vitro:
  LSZ-102 causes significant degradation of ERα after 24 h when given as a 10 μM solution to MCF-7 cells. LSZ-102 currently in Phase I/Ib trials for the treatment of ERα positive breast cancer. 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 show that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 (IC50: 0.3 nM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LSZ 102, LSZ102, LSZ-102, EstrogenReceptor, estrogen receptor, Estrogen Receptor, ERR

Compound Identifiers

PubChem CID

118574930