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EBI-2511
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EBI-2511图片
CAS NO:2098546-05-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 576.78
Formula C34H48N4O4
CAS No. 2098546-05-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1 mg/mL
Ethanol: <1 mg/mL
Chemical NameN-((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
SynonymsEBI-2511; EBI 2511; EBI2511
实验参考方法
In Vitro

In vitro activity: EBI-2511 is a novel and orally available benzofuran derived EZH2 inhibitors that was discovered through a scaffold hopping approach based on the clinical compound of EPZ-6438. It has the potential for treatment of Non-Hodgkin’s Lymphoma. Further rational structure-activity relationship exploration and optimization led to the discovery of more potent EZH2 inhibitors with oral bioavailability in mice and rats. EBI-2511 demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations.


Kinase Assay: EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.


Cell Assay: 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.

In VivoEBI-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
Animal model Pfeiffer tumor Xenograft models in mouse
Formulation & Dosage 10, 30, 100 mg/kg; Oral
References ACS Med Chem Lett. 2018 Jan 29;9(2):98-102.