| Bioactivity | Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells[1]. | ||||||||||||
| Invitro | Tazemetostat (EPZ-6438) 抑制多种野生型和突变型淋巴瘤细胞系增殖，IC50 为 0.49 nM-7.6 μM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Tazemetostat 相关抗体: Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | Tazemetostat (EPZ-6438；250 或 500 mg/kg，每天两次，持续 21-28 天) 几乎可以消除快速生长的 G401 肿瘤[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
| CAS | 1403254-99-8 | ||||||||||||
| Formula | C34H44N4O4 | ||||||||||||
| Molar Mass | 572.74 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Tazemetostat
CAS: 1403254-99-8 F: C34H44N4O4 W: 572.74
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity o
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