Tazemetostat

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Chemical Structure| 1403254-99-8 同义名 : EPZ-6438; E7438; E-7438
CAS号 : 1403254-99-8
货号 : A223202
分子式 : C34H44N4O4
纯度 : 98%
分子量 : 572.74
MDL号 : MFCD24849415
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(52.38 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

0.1 M HCL: 15 mg/mL(26.19 mM)，配合低频超声，并调节pH至5
生物活性
靶点

  • Histone Methyltransferase

    EZH2, IC50:11 nM

    EZH2, Ki:2.5 nM
描述 Tazemetostat (EPZ-6438) is a potent, selective, and orally available EZH2 inhibitor. It inhibits human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM and inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat also inhibits rat EZH2 with an IC50 of 4 nM and inhibits EZH1 with an IC50 of 392 nM. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells [1].
作用机制 EPZ-6438 inhibits EZH2 in a manner competitive with the substrate S-adenosylmethionine (SAM) binding to EZH2.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human HeLa cells Function assay 72 h Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method, IC50=0.02 μM. 26189078
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.75mL

0.35mL

0.17mL

8.73mL

1.75mL

0.87mL

17.46mL

3.49mL

1.75mL
参考文献

[1]Knutson SK, et, al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.