AGI-43192

AGI-43192 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that limitedly penetrates the blood-brain barrier. AGI-43192 exhibits inhibitory activitity against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC50s of 32 and 14 nM. AGI-43192 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-43192 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer[1].

Product Specifications

CAS Number

[2377491-54-6]

UNSPSC

12352005

Target

Methionine Adenosyltransferase (MAT)

Type

Reference compound

Related Pathways

Epigenetics; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/agi-43192.html

Concentration

10mM

Purity

99.47

Solubility

DMSO : 13.89 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1C(C2=CC=C(Cl)C=C2)=C3N=C(NCC(F)(F)F)N=CC3=CN1C4=CC5=CN(C)N=C5C=C4

Molecular Formula

C23H16ClF3N6O

Molecular Weight

484.86

References & Citations

[1] Li M, et al. Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads. J Med Chem. 2022;65 (6) :4600-4615.