NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC50 = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC50 = 5 nM). It can also inhibit the insulin-like growth factor 1 receptor (IC50 = 0.16 µM) as well as the activity of its downstream target genes such as MAPK and Akt. NVP-TAE226 has been shown to inhibit glioma and ovarian tumor growth in in vivo tumor models.