EBI-2511

EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC₅₀ of 6 nM in Pfeffiera cell lines, respectively. IC50 & Target: IC50: 6 nM (EZH2)^[1]. In Vitro: EBI-2511 (Compound 34) significantly reduces cellular H3K27me3 levels in a dose-dependent manner with an approximate IC₅₀ of 8 nM, which is 3-fold more potent than EPZ-6438. In addition to Pfeffier cell line, EBI-2511 was shown active with IC₅₀ value of 55 nM against WSU-DLCL2^[1]. In Vivo: EBI-2511 displays a dose-dependent inhibition on the tumor growth, resulting in 28% (10mg/kg), 83% (30mg/kg), and 97% (100mg/kg) reduction in tumor size. At the same dosage level, EBI-2511 shows a superior anti-tumor efficacy to EPZ-6438 (P<0.01). It is noteworthy that no significant changes in body weights of all treatment groups are observed^[1].