AG-270 (AG270) is a highly potent, selective, orally bioavailable methionine adenosyltransferase 2A (MAT2A) inhibitor with IC50 of 14 nM.
AG-270 demonstrated potent reduction in levels of intracellular SAM, as well as MTAP-null-selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro ((IC50=20 nM).
AG-270 (200 mg/kg q.d.) dose-dependently reduced tumor SAM levels and tumor growthpancreatic KP4 MTAP-null xenograft mouse model.
AG-270 showed excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey).
