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 In Vitro EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an K i value of 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice Dosage: 125, 250, 500, and 1000 mg/kg Administration: Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days Result: Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. Observed complete ablation of the methyl mark by the end of day 7. Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time. Animal Model: Rat Dosage: 30, 100, and 300 mg/kg Administration: Oral, single Result: dose (mg/kg) route t 1/2 (h) t max (h) C max (ng/mL) AUC inf (h*ng/mL) time above LCC (h) 30 p.o. 4.7 2 240 970 4 100 p.o. 3.9 2.7 1600 5600 8 300 p.o. 3.7 2.7 2900 10000 10 Form:Solid IC50& Target:EZH2

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