A MAT2A inhibitor
AG-270 is an inhibitor of methionine adenosyltransferase 2A (MAT2A; IC50 = 0.014 ?M).1 It reduces levels of S-(5'-adenosyl)-L-methonine in, and inhibits the proliferation of, HCT116 cells with a homozygous deletion of MTAP, the gene encoding methylthioadenosine phosphorylase (IC50s = 0.2 and 0.257 ?M, respectively). AG-270 (200 mg/kg) reduces intratumor SAM levels and tumor growth in KP4 and HCT116 MTAP-null, but not HCT116 MTAP-wild-type, mouse xenograft models.
1.Konteatis, Z., Travins, J.G., S., Marjon, K., et al.Discovery of AG-270, a first-in-class oral MAT2A inhibitor for the treatment of tumors with homozygous MTAP deletionJ. Med. Chem.64(8)4430-4449(2021)
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