TAE-226

TAE-226 is a small molecule, ATP-competitive multi-kinase inhibitor that primarily targets Focal Adhesion Kinase (FAK) and Proline-rich tyrosine kinase 2 (Pyk2). Developed by Novartis, it was one of the first FAK inhibitors to enter clinical evaluation. Beyond its primary targets, TAE-226 also demonstrates inhibitory activity against the Insulin-like Growth Factor 1 Receptor (IGF-1R) and Anaplastic Lymphoma Kinase (ALK). Preclinical research has shown that TAE-226 effectively suppresses tumor cell proliferation, invasion, and survival signaling pathways, including the AKT/mTOR and MAPK/ERK cascades, in various malignancies such as glioblastoma, esophageal squamous cell carcinoma, and gastric cancer. Although it showed potent antitumor efficacy in xenograft models, its clinical development was hampered by off-target toxicities, most notably hyperglycemia resulting from the inhibition of IGF-1R. Currently, TAE-226 is widely used as a reference compound and a structural scaffold for the development of next-generation FAK inhibitors with improved selectivity and pharmacological profiles.

Other names

2-({5-CHLORO-2-[(2-METHOXY-4-MORPHOLIN-4-YLPHENYL)AMINO]PYRIMIDIN-4-YL}AMINO)-N-METHYLBENZAMIDE2-[5-chloro-2-[2-methoxy-4-(4-morpholinyl)phenylamino]pyrimidin-4-ylamino]-N-methylbenzamideNVP-TAE226NVP-TAE-226NVP-TAE 226CHEMBL458997CHEMBL-458997CHEMBL 458997761437-28-9