EZH2-IN-4 is an orally active, potentEZH2inhibitor withIC₅₀s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer)EZH2and mutant 5-merEZH2, respectively. EZH2-IN-4 has anti-cancer activity^[1].

EZH2-IN-4 (example 38) shows a cell H3K27me3 IC₅₀of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells^[1].
EZH2-IN-4 shows an IC₅₀of 10.1 nM in Plate Kj<[1].
EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC₅₀s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC₅₀>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].

511.72

C₂₉H₄₁N₃O₃S

2088132-99-2

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