AGI-25696
AGI-25696 is an orally active ethionine adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 97 nM. AGI-25696 reduces intracellular SAM levels in cancer cells. AGI-25696 inhibits tumor growth in mice bearing subcutaneous KP4 MTAP-null pancreatic xenografts. AGI-25696 can be used for the research of mtap-deleted pancreatic cancer.
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- CAS No.: 2201065-84-9
- Formule: C28H20N4O
- Masse moléculaire:428.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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MAT2A 97 nM (IC50) |
AGI-25696 potently inhibits purified recombinant MAT2A homodimer with an IC50 of 97 nM[1].
AGI-25696 (72 h) dose-dependently reduces intracellular SAM levels in HCT116 MTAP-null cells with an IC50 of 150 nM and 84% maximal inhibition after 72 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice bearing subcutaneous KP4 MTAP-null
xenografts[1] -
Dosage:300 mg/kg
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Administration:p.o.; once daily; 33 days
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Result:Achieved a tumor growth inhibition (TGI) of 67.8% relative to vehicle-treated controls.
Caused no adverse effects on mouse body weight during the 33-day study.
Chemical Information
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CAS No. 2201065-84-9
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Masse moléculaire 428.48
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Formule C28H20N4O
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SMILES
O=C1C(C2=CC3=C(N=CC=C3)C=C2)=C(C)NC4=C(C(C5=CC=CC=C5)=NN14)C6=CC=CC=C6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)