AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC 50 of 14 nM In Vitro AG-270 demonstrates potent reduction in levels of intracellular SAM , as well as MTAP-–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro. AG-270 exhibits an IC 50 of 20 nM in HCT116 MTAP- cell SAM at 72 h. MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo AG-270 shows excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey). AG-270 exhibits T1/2 values of 5.9 h, 4.2 h, 4.8 h and 21.3 h in mouse, rat, monkey and dog, respectively . AG-270 (200 mg/kg, orally, q.d. for 38 days) results in dose-dependent reduction in tumor SAM levels and tumor growth of KP4 MTAP- xenografts and is well tolerated, with mean body weight loss IC50& Target:IC50: 14 nM (MAT2A)
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AG-270
CAS number：2201056-66-6(DMSO) molecular formula：C30H27N5O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2201056-66-6(DMSO) | molecular formula | C30H27N5O2 |
| molecular weight | 489.57 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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