YM458

Powder: -20 degree C for 3 years | In solvent: -80 degree C for 1 year

957.62

C53H61ClN8O5S

(< 1 mg/ml refers to the product slightly soluble or insoluble)

2770108-93-3

EZH2: 490 nM, BRD4: 34 nM

YM458 administered intraperitoneally (IP; 60 mg/kg; every other day, for 38 days) exhibited anticancer activity by inhibiting tumor growth in AsPC-1 and A549 cells, with rates of 38.6% and 62.3%, respectively [1]. In female BALB/c mice, pharmacokinetic parameters revealed after IP administration (80 mg/kg), YM458 had a half-life (t1/2) of 3.81 hours and reached its maximum concentration (Cmax) of 27126.3 ng/mL within 1 hour (Tmax), while oral administration (PO) of the same dosage resulted in a longer half-life (4.16 hours), lower peak concentration (4383.6 ng/mL), and a substantially reduced area under the curve (AUC 0-24) of 13509.1 ng/mL·h. The clearance rate (CL) was 4.88 mL/min/kg with an oral bioavailability (F) of 4.94% [1].