GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™,10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Argon charged,Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Overview
LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC 50 of 0.2 nM.
In Vitro
LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC 50 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 IC 50 of 0.3 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:estrogen receptor
Specifications
Specifications & Purity
Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms
LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC 50 of 0.2 nM.
Storage
Argon charged, Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
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