EZH2-IN-4
Names
[ CAS No. ]:
2088132-99-2
[ Name ]:
EZH2-IN-4
Biological Activity
[Description]:
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s 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[1].
[Related Catalog]:
[Target]
WT 5-mer EZH2:0.923 nM (IC50)
mut 5-mer EZH2:2.65 nM (IC50)
[In Vitro]
EZH2-IN-4 (example 38) shows a cell H3K27me3 IC50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1]. EZH2-IN-4 shows an IC50 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; IC50s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC50>20 μM)[1].
[In Vivo]
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].
[References]
Chemical & Physical Properties
No Any Chemical & Physical Properties
Related Compounds
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