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AG-270

CAS No. : 2201056-66-6

MCE 国际站：AG-270

产品活性：AG-270 是非竞争性的、首创的、可逆的、具有口服活性的 MAT2A 变构抑制剂，其 IC₅₀ 值为 14 nM。

研究领域：Epigenetics  |  Metabolic Enzyme/Protease

作用靶点：Methionine Adenosyltransferase (MAT)

In Vitro: AG-270 demonstrates potent reduction in levels of intracellular SAM, as well as MTAP-null–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro.
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).

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-null xenografts and is well tolerated, with mean body weight loss <5%.
Combining AG-270 with taxanes and gemcitabine yielded additive-tosynergistic antitumor activity, with the docetaxel combination yielding 50% complete tumor regressions in select models; combination benefits are observed in PDX models derived from esophageal, NSCLC, and pancreatic cancers.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Chemical Probe Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  AGI-25696  |  MAT2A inhibitor 2  |  MAT2A-IN-10  |  MAT2A inhibitor 3  |  MAT2A inhibitor 4  |  FIDAS-5  |  PF-9366  |  AGI-24512  |  MAT2A inhibitor 1  |  MAT2A-IN-9

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