EZH2-IN-4

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

EZH2-IN-4 

EZH2-IN-4 是一种口服有效的 EZH2 抑制剂,对野生型和突变型 5-mer EZH2 的 IC50 分别为 0.923 nM 和 2.65 nM。EZH2-IN-4 具有抗癌活性。

EZH2-IN-4

EZH2-IN-4 Chemical Structure

CAS No. : 2088132-99-2

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生物活性

EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity[1].

IC50 & Target[1]

WT 5-mer EZH2

0.923 nM (IC50)

mut 5-mer EZH2

2.65 nM (IC50)

体外研究
(In Vitro)

EZH2-IN-4 (example 38) shows a cell H3K27me3 IC50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1].
EZH2-IN-4 shows an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1].
EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC50s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC50>20 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1].
EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

511.72

Formula

C29H41N3O3S

CAS 号

2088132-99-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Esteban DOMINGUEZ, et al. Inhibitors of ezh2. WO2017035060A1.

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