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AG-270 

Cat. No.: HY-138630
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AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.

For research use only. We do not sell to patients.

AG-270 Chemical Structure

AG-270 Chemical Structure

CAS No. : 2201056-66-6

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Description

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM[1].

IC50 & Target

IC50: 14 nM (MAT2A)[1].

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[1].
AG-270 exhibits an IC50 of 20 nM in HCT116 MTAP-null cell SAM at 72 h[1].
MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM)[2].

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[1].
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%[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pancreatic KP4 MTAP-null xenograft mouse model[1].
Dosage: 10-200 mg/kg.
Administration: Orally, q.d. for 38 days.
Result: Led to dose-dependent reductions in tumor SAM levels and tumor growth of KP4 MTAP-null xenografts (TGI = 36% (10 mg/kg), 48% (30 mg/kg), 66% (100 mg/kg), 67% (200 mg/kg).
Clinical Trial
Molecular Weight

489.57

Formula

C₃₀H₂₇N₅O₂

CAS No.
SMILES

O=C1C(C2=CC=C(OC)C=C2)=C(NC3=NC=CC=C3)NC4=C(C5=CCCCC5)C(C6=CC=CC=C6)=NN14

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

AG-270AG270AG 270OthersLowtoxicitypancreaticcancerSAMsolidtumorlymphomaInhibitorinhibitorinhibit

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