EBI-2511

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EBI-2511 是一种高效且具有口服活性的 EZH2 抑制剂，针对突变型 EZH2 A677G 的 IC50 为 4 nM。

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; dose-dependently inhibits tumor growth at 10-100 mg/kg, po., shows a superior anti-tumor efficacy to EPZ-6438 in Pfeiffer Xenograft mouse model.

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.

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.

EBI2511

Chromatin/Epigenetic

HMTase

HMTase

Cancer

——

2098546-05-3

576.782

C34H48N4O4

>98% (HPLC)

DMSO : 5 mg/mL 8.67 mM

O=C(C1=C2C=C(C3CCN(C(C)C)CC3)OC2=CC(N(CC)C4CCOCC4)=C1CC)NCC5=C(C)C=C(C)NC5=O

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-ethyl-6-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-(1-isopropylpiperidin-4-yl)benzofuran-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years