Chemical Structure : IDE397
CAS No.: 2439277-80-0
Catalog No.: PC-21894Not For Human Use, Lab Use Only.
Tuvutromstat (IDE397, GSK4362676, 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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Tuvutromstat (IDE397, GSK4362676, 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.
| M.Wt | 340.69 | |
| Formula | C14H8ClF3N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Pyrido[2,3-d]pyrimidin-2(1H)-one, 4-amino-1-(2-chlorophenyl)-7-(trifluoromethyl)- |
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1. Marcus M. Fischer, et al. Cancer Res (2021) 81 (13_Supplement): 1278. 2. Zihan Shi, et al. J Med Chem. 2025 Nov 27;68(22):24213-24231. 3. Patent WO2022256808 A1 2022-12-08.

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