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Cat. No.: HY-182400

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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.

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

CAS No.: 2201065-84-9
Formula: C₂₈H₂₀N₄O
Molecular Weight:428.48

Storage:

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

AGI-25696 Chemical Structure

CAS No.: 2201065-84-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

MAT2A

97 nM (IC₅₀)

In Vitro

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.

In Vivo

AGI-25696 (300 mg/kg; p.o.; once daily; 33 days) achieves a tumor growth inhibition of 67.8% in mice bearing subcutaneous KP4 MTAP-null pancreatic xenografts, with no observed body weight loss^[1].

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

Animal Model:

Mice bearing subcutaneous KP4 MTAP-null
xenografts^[1]
Dosage:

300 mg/kg
Administration:

p.o.; once daily; 33 days
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

CAS No. 2201065-84-9
Molecular Weight 428.48
Formula C₂₈H₂₀N₄O
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Konteatis Z, et al. Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion. J Med Chem. 2021;64(8):4430-4449. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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