| Hazard Information | Back Directory | [Description]
LSN3346149 is a novel Enhancer of Zeste Homolog 2 (EZH2). | [Uses]
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity[1]. | [in vivo]
EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1].
EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].
| [IC 50]
WT 5-mer EZH2: 0.923 nM (IC50); mut 5-mer EZH2: 2.65 nM (IC50) | [References]
[1] Esteban DOMINGUEZ, et al. Inhibitors of ezh2. WO2017035060A1. |
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