In Vitro: Antitumor agent-101 (Compound 27) ( 0-5 μM; 48 hours) significantly exhibits proliferation and colony formation of PANC-1 and MDA-MB-231 cells with IC50s of 2.68 and 2.88 μM, respectively. Antitumor agent-101 (0-10 μM; 0-96 hours) effectively reduces H3K9me2 in PANC-1 and MDA-MB-231 cells in a concentration- and time-dependent manner.
In Vivo: Antitumor agent-101 (Compound 27) (2 mg/kg for i.p., 5 days a week) suppresses PANC-1 xenograft tumor growth by inhibiting the methyltransferase activity of G9a/GLP. Antitumor agent-101 (2 mg/kg for p.o.) shows a Cmax of 316 ng/mL, and mean residence time (MRT) of 0.61 hour.