TAE226 (NVP-TAE226)

Description

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.

Uses

NVP-TAE 226 is FAK and IGF-IR inhibitor. It can be used in biological study and therapeutic use of TAE226, a bis-?anilino pyrimidine compound, inhibits the egfr-?mutant kinase including T790M mutant to show anti-?tumor effect on EGFR-?mutant non-?small cell lung cancer cells.

Definition

ChEBI: 2-[[5-chloro-2-[2-methoxy-4-(4-morpholinyl)anilino]-4-pyrimidinyl]amino]-N-methylbenzamide is a member of morpholines.

in vivo

target

PYK2

References

[1]. liu, t.j., et al., inhibition of both focal adhesion kinase and insulin-like growth factor-i receptor kinase suppresses glioma proliferation in vitro and in vivo. mol cancer ther, 2007. 6(4): p. 1357-67.
[2]. plaza-menacho, i., et al., focal adhesion kinase (fak) binds ret kinase via its ferm domain, priming a direct and reciprocal ret-fak transactivation mechanism. j biol chem, 2011. 286(19): p. 17292-302.