EPZ005687
Cat. No.:YN310271
CAS No. :1396772-26-1
产品名称: | EPZ005687 |
CAS No.: | 1396772-26-1 |
Chemical Name: | 1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide |
Synonyms: | EPZ005687;1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide;1H-Indazole-4-carboxamide, 1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)pheny |
分子量: | 539.67 |
分子式: | C₃₂H₃₇N₅O₃ |
SMILES: | O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=CC5=C2C=NN5C6CCCC6 |
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: | EPZ005687 是一种有效的,选择性的EZH2抑制剂,Ki值为 24 nM,对其选择性是对 EZH1 的 50 倍,对其他 15 种甲基转移酶的 500 倍。 |
IC50和靶点: | [{name:"EZH2:24 nM (Ki)"}] |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Knutson, S.K., Wigle, T.J., Warholic, N.M., et al.A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cellsNat. Chem. Biol.8(11),890-896(2012)
Wigle, T.J., and Copeland, R.A.Drugging the human methylome: An emerging modality for reversible control of aberrant gene transcriptionCurr. Opin. Chem. Biol.17(3),369-378(2013)
Konze, K.D., Ma, A., Li, F., et al.An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1ACS Chem. Biol.8(6),1324-1334(2013)