Product Details
| Product Name: LSZ-102 | CAS No.: 2135600-76-7 |
| Min. Order: 1kg | Purity: 99% |
| Supply Ability: 100kg | Release date: 2025/10/13 |
| Lead time: in stock | Packaging: bag/bottle/drum//IBC, as request |
| Delivery: By sea, by air, by express | Origin: Manufacturer, advantage products |
| COA, MSDS: Available, contact us for details | Contact: Tina |
PRODUCT INFORMATION
| Name | LSZ-102 |
|---|
| Description | LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM. |
|---|---|
| Related Catalog | Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer |
| Target | estrogen receptor[1] |
| 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[1]. |
| 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[1]. |
| Kinase Assay | Growth factors depleted MCF-7 ERE-luc cells are used and seeded (10 000 cells/well) in 96-well plates in CSS medium. After overnight incubation, cells are treated with LSZ-102 in the presence of estradiol (0.1 nM) for 24 h. Cells are then lysed and quantified for luciferase activity using Bright-Glo assay[1]. |
| Animal Admin | Female athymic nude mice are used for tumor xenograft studies. MCF-7 cells are subcutaneously injected (200 μL/animal) in the right axillary mammary fat pad area. Tumor volume and body weights are measured twice weekly. When tumors reach an average volume of ~200 mm3, mice are randomized into different groups. Animals are orally administered vehicle alone or 20 mg/kg LSZ-102 daily or 60 mg/kg tamoxifen 5 days per week[1]. |
| References | [1]. Tria GS, et al. Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. J Med Chem. 2018 Apr 12;61(7):2837-2864. |
| Molecular Formula | C25H17F3O4S |
|---|---|
| Molecular Weight | 470.46 |
| Storage condition | 2-8℃ |
Company Profile
Our company is a high-tech enterprise specializing in chemical raw materials such as electronic materials, optoelectronic materials, semiconductor materials, UV monomers, silane catalysts, cosmetic raw materials, etc. The company integrates research and development, production, customized synthesis, and sales, and is committed to providing customers with high-quality chemical product solutions.
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Our products have been exported to many countries, including Germany, Spain, the United Kingdom, the United States, Australia, the Middle East, Asia, and more. We have received highly positive feedback from our clients and have established long-term friendly cooperative relationships with them.
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Contact name: Tina
Email address: Tina@fdachem.com
Mob: 86 13213167925
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Company Profile Introduction
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