[CAS NO. 761437-28-9]  NVP-TAE226

NVP-TAE 226 (TAE226), a potent ATP-competitive inhibitor of several tyrosine protein kinases, in particular FAK and IGF-IR kinases. In a cell-based kinase assays, FAK, IGF-IR kinase, and IR kinase are inhibited with an IC ₅₀ range of 100 to 300 nM compared with the other kinases tested, which are >10-fold less sensitive. In culture, NVP-TAE 226 inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr ³⁹⁵ ). NVP-TAE 226 also inhibits IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt . NVP-TAE 226 retards tumor cell growth as assessed by a cell viability assay and attenuates G ₂ -M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr ¹⁵ ) protein expression. NVP-TAE 226 treatment inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay. Interestingly, TAE226 treatment of tumor cells containing wild-type p53 mainly exhibits G ₂ -M arrest, whereas tumor cells bearing mutant p53 underwent apoptosis ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.