EPZ011989
目录号: PL15058 纯度: ≥99%
CAS No. :1598383-40-4
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中文名称
EPZ011989
中文别名
EPZ011989
英文名称
EPZ011989
英文别名
EPZ011989
Cas No.
1598383-40-4
分子式
C35H51N5O4
分子量
605.81
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
EPZ011989 是一种有效且代谢稳定的 Zeste Homolog 2 (EZH2) 抑制剂,具有口服活性。EPZ011989 对 EZH2 具有抑制性抑制作用,Ki 值 <3 nM。EPZ011989 具有出强大的甲基标记抑制和抗肿瘤活性。EPZ011989 可用于多种癌症的研究。
生物活性
EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a K i value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers.
性状
Solid
IC50 & Target[1][2]
Ki: <3 nM (EZH2); IC50: 94 nM (H3K27 methylation inhibition).
体外研究(In Vitro)
EPZ011989 inhibits mutant and wild-type EZH2 with an Ki value of <3 nM.
EPZ011989 reduces cellular H3K27 methylation with an IC50 value of 94 nM.
EPZ011989 (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
EPZ011989 (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.
溶解度数据
In Vitro: DMSO : 100 mg/mL (165.07 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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