EPZ011989 (trifluoroacetate)

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 K_i 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, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target:Ki: <3 nM (EZH2); IC50: 94 nM (H3K27 methylation inhibition)^[1]. In Vitro: EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an K_i 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]. In Vivo: 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].