EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC 50 s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.

EZH2-IN-4 (example 38) shows a cell H3K27me3 IC 50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1]. EZH2-IN-4 shows an IC 50 of 10.1 nM in Plate Kj?pas-422 cells[1]. EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC 50 s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC 50 >20 μM)[1].

EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1]. EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].

2088132-99-2

C29H41N3O3S

511.73

EZH2-IN-4

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years