For research use only. Not for therapeutic Use.
EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers[1]. EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an Ki value of <3 nM[1].
EPZ-011989 trifluoroacetate reduces cellular H3K27 methylation with an IC50 value of 94 nM[1].
EPZ-011989 trifluoroacetate (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells[1].
EPZ-011989 trifluoroacetate (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity[1].
| Catalog Number | I002026 |
| CAS Number | 1598383-41-5 |
| Synonyms | N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl-[4-[2-methoxyethyl(methyl)amino]cyclohexyl]amino]-2-methyl-5-(3-morpholin-4-ylprop-1-ynyl)benzamide;2,2,2-trifluoroacetic acid |
| Molecular Formula | C37H52F3N5O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C35H51N5O4.C2HF3O2/c1-7-40(30-12-10-29(11-13-30)38(5)15-18-43-6)33-23-28(9-8-14-39-16-19-44-20-17-39)22-31(27(33)4)34(41)36-24-32-25(2)21-26(3)37-35(32)42;3-2(4,5)1(6)7/h21-23,29-30H,7,10-20,24H2,1-6H3,(H,36,41)(H,37,42);(H,6,7) |
| InChIKey | JAUQBEFSKUVFDO-UHFFFAOYSA-N |
| SMILES | CCN(C1CCC(CC1)N(C)CCOC)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C#CCN4CCOCC4.C(=O)(C(F)(F)F)O |
| Reference | [1]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495. |
