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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
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

产品介绍
EBI-2511是具有口服活性的、EZH2的有效抑制剂,其在Pfeffiera细胞中的IC50值为6nM。
Cas No.2098546-05-3
Canonical SMILESCCC1=C(C(NCC2=C(C)C=C(C)NC2=O)=O)C(C=C(C3CCN(C(C)C)CC3)O4)=C4C=C1N(C5CCOCC5)CC
分子式C34H48N4O4
分子量576.77
溶解度DMSO : 5 mg/mL (8.67 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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

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].

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].

[1]. Lu B, et al. Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma. ACS Med Chem Lett. 2018 Jan 29;9(2):98-102.