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IDE-397

Chemical Structure : IDE-397

CAS No.: 2439277-80-0

IDE-397 (GSK-4362676, GSK-676, IDE397)

Catalog No.: PC-21894Not For Human Use, Lab Use Only.

IDE-397 (GSK-4362676, GSK-676) is a potent, selective small molecule methionine adenosyltransferase 2a (MAT2A) inhibitor, displays broad anti-tumor activity across a panel of MTAP-deleted patient-derived xenografts.

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Biological Activity

IDE-397 (GSK-4362676, GSK-676) is a potent, selective small molecule methionine adenosyltransferase 2a (MAT2A) inhibitor, displays broad anti-tumor activity across a panel of MTAP-deleted patient-derived xenografts.
IDE397 produces a dose- and time-dependent modulation of the proximal and distal PD biomarkers SAM and symmetrically di-methylates arginine (SDMA) in HCT116 MTAP-deleted CDX model.
HCT116 MTAP-deleted CDX model is more sensitive to IDE397 compared to the HCT116 MTAP-WT model.
IDE397 displays broad anti-tumor activity across a panel of MTAP-deleted patient-derived xenografts. exhibits anti-tumor activity as a single agent in MTAP-deleted CDX models and in MTAP-deleted PDX models of NSCLC, pancreatic, bladder, head and neck, esophageal and gastric cancer.

Physicochemical Properties

M.Wt 340.69
Formula C14H8ClF3N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Pyrido[2,3-d]pyrimidin-2(1H)-one, 4-amino-1-(2-chlorophenyl)-7-(trifluoromethyl)-

References

1. Marcus M. Fischer, et al. Cancer Res (2021) 81 (13_Supplement): 1278.

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