9- [5-脱氧-5-[[顺-3- [2- [6-（1,1-二甲基乙基）-1H-苯并咪唑-2-基]乙基]环丁基]（1-甲基乙基）氨基]-β -D-呋喃核糖基] -9H-嘌呤-6-胺 CAS:152914-63-1

背景资料

DOT1L is a non-SET domain containing methyltransferase whose function is important for the transcriptional activation of certain genes, DNA damage repair, and cell cycle regulation. DOT1L is known to play an essential role in MLL-rearranged leukemias, and thus has emerged as a drug target for these leukemias.{21198,21195} EPZ5676 is a highly potent aminonucleoside inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) that demonstrates 37,000-fold selectivity over other methyltransferases.{26366,26367} In various human leukemia cell lines, EPZ5676 has been shown to inhibit the methylation of lysine 79 on histone 3 (IC50s = 3-5 nM), decreasing MLL-fusion target gene expression (IC50s = 53-67 nM).{26366} It can selectively inhibit the proliferation of acute leukemia cell lines bearing MLL translocations (IC50s range from 3.5 nM - 1.3 µM).{26366} Continuous intravenous infusion of EPZ5676 at a dose of 35 mg/kg has been reported to cause complete and sustained tumor regression in a rat xenograft model of MLL-rearranged leukemia.{26366}

保存条件

建议您在收到Cayman Chemical品牌的EPZ5676 (10 mg)产品后置于-20度保存，产品有效期为730天.

品牌介绍

Cayman Chemical向全球科学工作者提供多研究领域的生化、免疫试剂和分析试剂盒，其产品被广泛应用于肿瘤、氧化氮、神经学、凋亡、氧化性损伤、内分泌学等不同研究领域.Cayman Chemical可提供用于检测的特色试剂盒，如：类花生酸类物质、游离的生物标志、环核苷、激素及氧化氮等；也提供多种高质量试剂，包括：类花生酸类物质、氧化氮试剂及许多相关脂质、脂肪酸、酶和抗体.作为Cayman Chemical在中国的区域总代理，艾美捷科技有限公司将为中国客户提供最全面的Cayman Chemical产品以及客户订制化服务.

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