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AG-270 is a non-competitive, first-of-its-kind, reversible, orally active MAT2A allogeneic inhibitor IC50 The value is 14 nM. AG-270 exhibits an IC50 of 20 nM in HCT116 MTAP-null 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).
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-null xenografts and is well tolerated, with mean body weight loss <5%.
| Molecular Weight | 489.57 |
| Formula | C30H27N5O2 |
| CAS Number | 2201056-66-6 |
| Solubility (25°C) | DMSO 4 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Methionine Adenosyltransferase Products |
|---|
| PF-9366
PF-9366 is a novel inhibitor of human methionine adenosyltransferase 2A (Mat2A), with IC50 of 420 nM and Kd of 170 nM. |
| FIDAS-5
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. |
| IDE397
IDE397 (GSK-4362676) is a potent, potential "first-in-class" inhibitor of methionine adenosyltransferase 2A (MAT2A). IDE397 (GSK-4362676) exhibits anti-tumor activity in MTAP-deleted PDX models. |
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