AGI-24512 Chemical Properties

Boiling point:

639.3±65.0 °C(Predicted)

Density 

1.33±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 125 mg/mL (312.13 mM);Water : < 0.1 mg/mL (insoluble)

pka

9.47±0.30(Predicted)

form 

Solid

color 

White to gray

AGI-24512 Usage And Synthesis

Description

AGI-24512 is a MATA2 inhibitor that are useful as therapeutic agents for treating malignancies. AGI-24512 showed in vivo activity in MTAP null tumors.

Uses

AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer[1].

in vivo

References

[1] Kalev P, et al. MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage. Cancer Cell. 2021 Feb 8;39(2):209-224.e11. DOI:10.1016/j.ccell.2020.12.010
[2] 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 Apr 22;64(8):4430-4449. DOI:10.1021/acs.jmedchem.0c01895