Product Details
| Product Name: LSZ-102 | CAS No.: 2135600-76-7 |
| Min. Order: 1kg | Purity: 99% |
| Supply Ability: 100kg | Release date: 2026/04/17 |
| 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℃ |
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