产品名称

英文名称：EPZ005687

同义词

EPZ005687、1396772-26-1、EPZ-005687、1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide、EPZ 005687、1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmet

产品性质

CAS编号：1396772-26-1

分子式：C32H37N5O3

分子量：539.67

PubChem编号：60160561

英文别名：EPZ005687|1396772-26-1|EPZ-005687|1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide|EPZ 005687|1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmet

规格或纯度：≥98%

英文名称：EPZ005687

生化机理：EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2) and is involved in repressing gene expression throμgh methylation of histone H3 on lysine 27 (H3K27). EZH2 overexpression is implicated in tumorigenesis and correlates with poor prognosis in several tumour types. EPZ005687, a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：卖完停产，不再备货

产品介绍：EPZ005687是一种有效的，选择性EZH2抑制剂，Ki为24 nM，比作用于EZH1选择性高50倍，比作用于15种其他蛋白甲基转移酶选择性高500倍。EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases

IUPAC Name：1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide

INCHI：InChI=1S/C32H37N5O3/c1-21-15-22(2)35-32(39)28(21)18-33-31(38)27-16-25(17-30-29(27)19-34-37(30)26-5-3-4-6-26)24-9-7-23(8-10-24)20-36-11-13-40-14-12-36/h7-10,15-17,19,26H,3-6,11-14,18,20H2,1-2H3,(H,33,38)(H,35,39)

InChi Key：ZOIBZSZLMJDVDQ-UHFFFAOYSA-N

Canonical SMILES：CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC=C(C=C4)CN5CCOCC5)C6CCCC6)C

Isomeric SMILES：CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC=C(C=C4)CN5CCOCC5)C6CCCC6)C

PubChem CID：60160561

CAS Registry No.：1396772-26-1

溶解性：DMSO

产品包装