AGI-41998 (10 mg/kg, p.o., single dose) reduces the levels of tumor and brain S-adenosyl methionine (SAM) with EAUC50s of 9680 and 26400 h·ng/mL in mice bearing HCT-116 tumors with MTAP deficiency. AGI-41998 (30-60 mg/kg, p.o., once daily for 13 days) significantly inhibits tumor growth in KP4 xenograft mice models.