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 IC50& Target:estrogen receptor
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LSZ-102
CAS number：2135600-76-7(DMSO) molecular formula：C25H17F3O4S
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2135600-76-7(DMSO) | molecular formula | C25H17F3O4S |
| molecular weight | 470.46 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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