tae226-nvp-tae226

Description: TAE226 (also known as NVP-TAE226; TAE-226) is a novel, potent, selective and ATP competitive small molecule FAK (focal adhesion kinase) inhibitor with potential antineoplastic activity. It inhibits FAK with IC50 of 5.5 nM, shows modest potency against other kinases such as Pyk2, InsR, IGF-1R, ALK, and c-Met. TAE 226 demonstrate significant in vivo antitumor efficacy in Nude mice (male) bearing intracranial glioma xenografts. When tested with glioma cell lines U87, U87/EGFR, U87/EGFRvIII and U251 that expressed different level of FAK, TAE226 (NVP-TAE226) showed effective inhibition on the growth of the 4 cell lines in a dose dependent manner (1 and 10 umol/L) and U87/EGFR, as well as U87/EGFRvIII, which had higher p-FAK expression than U87 were more sensitive to TAE226 (NVP-TAE226).

References: Mol Cancer Ther. 2007 Apr; 6(4):1357-67; Invest New Drugs. 2010 Dec; 28(6):825-33.

Chemical Name: 2-((5-chloro-2-((2-methoxy-4-morpholinophenyl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide

InChi Key: UYJNQQDJUOUFQJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H25ClN6O3/c1-25-22(31)16-5-3-4-6-18(16)27-21-17(24)14-26-23(29-21)28-19-8-7-15(13-20(19)32-2)30-9-11-33-12-10-30/h3-8, 13-14H, 9-12H2, 1-2H3, (H, 25, 31)(H2, 26, 27, 28, 29)

SMILES Code: O=C(NC)C1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2Cl