EBI-2511 是一种高效且具有口服活性的 EZH2 抑制剂，在 Pfeffiera 细胞系中的IC50值为 6 nM。

EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines).

EBI-2511 obviously decreases cellular H3K27me3 levels in a dose-dependent manner (an approximate IC50: 8 nM) and it is 3-fold more potent than EPZ-6438. In addition to Pfeffier cell line, EBI-2511 was shown active against WSU-DLCL2 ( IC50: 55 nM) [1].

EBI-2511 shows a dose-dependent inhibition on the tumor growth, resulting in 28% (10mg/kg), 83% (30mg/kg), and 97% (100mg/kg) reduction in tumor size. There is no significant changes in body weights of all treatment groups are observed. At the same dosage level, EBI-2511 displays a superior anti-tumor efficacy to EPZ-6438 (P<0.01) [1].

2098546-05-3

C34H48N4O4

576.77

DMSO:5 mg/mL (8.67 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years