Tazemetostat
Cat. No.：YN310245
CAS No. ：1403254-99-8
| 产品名称: | Tazemetostat |
| CAS No.: | 1403254-99-8 |
| Chemical Name: | N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide |
| Synonyms: | EPZ-6438; E-7438 |
| 分子量: | 572.74 |
| 分子式: | C₃₄H₄₄N₄O₄ |
| SMILES: | O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Tazemetostat (EPZ-6438) 是一种有效，选择性，口服的EZH2抑制剂。Tazemetostat (EPZ-6438) 抑制含有 PRC2 复合体的野生型 EZH2 的活性，Ki值为 2.5±0.5 nM。Tazemetostat (EPZ-6438) 抑制 EZH2，在肽测定和核小体测定中 IC50分别为 11 和 16 nM。Tazemetostat (EPZ-6438) 抑制大鼠 EZH2，IC50为 4 nM。Tazemetostat (EPZ-6438) 还抑制 EZH1，IC |
| IC50和靶点: | |
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Knutson, S.K., Warholic, N.M., Wigle, T.J., et al.Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2Proc. Natl. Acad. Sci. USA110(19),7922-7927(2013)
Knutson, S.K., Kawano, S., Minoshima, Y., et al.Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphomaMol. Cancer Ther.13(4),842-854(2014)
