NVP-TAE 226

NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively[1][2].

Product Specifications

CAS Number

[761437-28-9]

Product Name Alternative

TAE226

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; FAK; IGF-1R; Insulin Receptor; Pyk2

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Endocrinology

Assay Protocol

https://www.medchemexpress.com/NVP-TAE-226.html

Purity

99.77

Solubility

DMSO : 11.11 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=C(C=CC=C1)NC2=NC(NC3=C(C=C(C=C3)N4CCOCC4)OC)=NC=C2Cl)NC

Molecular Formula

C23H25ClN6O3

Molecular Weight

468.94

Precautions

H302, H315, H319, H335

References & Citations

[1]Liu TJ, 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), 1357-1367.|[2]Delimont D, et al. Laminin α2-mediated focal adhesion kinase activation triggers Alport glomerular pathogenesis. PLoS One. 2014 Jun 10;9 (6) :e99083.|[3]Lietha D, et al. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS One. 2008;3 (11) :e3800.