AG-270

AG-270 is an inhibitor of methionine adenosyltransferase 2A (MAT2A, IC50 = 0.014 µM). It reduces levels of S-(5'-adenosyl)-L-methonine (SAM, Cay-16376, Cay-17595) 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 µM, 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.Formal Name: 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-pyrazolo[1,5-a]pyrimidin-7(4H)-one. CAS Number: 2201056-66-6. Molecular Formula: C30H27N5O2. Formula Weight: 489.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly soluble. lambdamax: 273, 317 nm. SMILES: O=C1C(C2=CC=C(OC)C=C2)=C(NC3=C(C4=CCCCC4)C(C5=CC=CC=C5)=NN13)NC6=CC=CC=N6. InChi Code: InChI=1S/C30H27N5O2/c1-37-23-17-15-21(16-18-23)26-28(32-24-14-8-9-19-31-24)33-29-25(20-10-4-2-5-11-20)27(34-35(29)30(26)36)22-12-6-3-7-13-22/h3,6-10,12-19,33H,2,4-5,11H2,1H3,(H,31,32). InChi Key: HSVRUECLQUGTDS-UHFFFAOYSA-N.