EBI-2511 is a highly potent and orally active EZH2 inhibitor with IC50 of 4 nM against mutant EZH2 A677G; significantly reduces cellular H3K27me3 levels in a dose-dependent with IC50 of 8 nM in Pfeffier cell line, IC50 of 55 nM against WSU-DLCL2.
EBI-2511 dose-dependently inhibits tumor growth at 10-100 mg/kg, po.
EBI-2511 shows a superior anti-tumor efficacy to EPZ-6438 in Pfeiffer Xenograft mouse model.
