Inhibition of EED ( 1 to 441 residues) (unknown origin) pre-incubated for 15 mins before biotin-H3K27me3 (19 to 33 residues) addition and further incubated for 30 mins by AlphaScreen.based EED-H3K27me3 peptide competition binding assay
Inhibition of EED in SCID mouse xenografted with human KARPAS422 cells assessed as reduction in H3K27me3 level in tumor at 100 mg/kg, po dosed as single administration measured after 24 hrs by Western blotting analysis
Antitumor activity against human KARPAS422 cells xenografted in SCID mouse assessed as induction of tumor regression at 50 mg/kg, po dosed daily for 28 days relative to control
Antitumor activity against human KARPAS422 cells xenografted in SCID mouse assessed as induction of tumor regression at 100 mg/kg, po dosed daily for 28 days relative to control
Antitumor activity against human KARPAS422 cells xenografted in SCID mouse assessed as reduction in tumor re-growth at 50 to 100 mg/kg, po dosed daily for 28 days followed by treatment cessation for 72 days relative to control
Potency index, ratio of IC50 for EED226 to IC50 for test compound for inhibition of EED ( 1 to 441 residues) (unknown origin) pre-incubated for 15 mins before biotin-H3K27me3 (19 to 33 residues) addition and further incubated for 30 mins by AlphaScreen.based EED-H3K27me3 peptide competition binding assay