For research use only, not for therapeutic use.
TAE-226 (Cat No.:I004818), also known as NVP-TAE226, is a potent inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (Pyk2) with IC50 values of 5.5 nM and 3.5 nM, respectively. It exhibits 10- to 100-fold less potency against insulin receptor (InsR), insulin-like growth factor-1 receptor (IGF-1R), anaplastic lymphoma kinase (ALK), and c-Met. In vitro, TAE-226 inhibits autophosphorylation of FAK and IGF-1R, as well as downstream signaling pathways, leading to the suppression of tumor cell growth, attenuation of cell cycle progression, and inhibition of tumor cell invasion. It induces G2-M cell cycle arrest and apoptosis in glioma cell lines, depending on their p53 status. TAE-226 also demonstrates anti-angiogenic activity by inhibiting tube formation. In vivo, TAE-226 increases the survival rate in glioma xenograft models and decreases microvessel density in a colon cancer model.
| Catalog Number | I004818 |
| CAS Number | 761437-28-9 |
| Synonyms | 2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]-N-methylbenzamide |
| Molecular Formula | C₂₃H₂₅ClN₆O₃ |
| Purity | ≥95% |
| Target | FAK |
| Solubility | DMSO 93.3 mg/ml; Water <1 mg/ml |
| Storage | 3 years -20C powder |
| IC50 | 5.5 nM (FAK); 3.5 nM (Pyk2) |
| IUPAC Name | 2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]-N-methylbenzamide |
| InChI | 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) |
| InChIKey | UYJNQQDJUOUFQJ-UHFFFAOYSA-N |
| SMILES | CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCOCC4)OC |
| Reference | </br>1:Draft Genome Sequences of Two <i>Streptococcus pneumoniae</i> Serotype 19A Sequence Type 226 Clinical Isolates from Hungary, Hu17 with High-Level Beta-Lactam Resistance and Hu15 of a Penicillin-Sensitive Phenotype. Rieger M, Denapaite D, Brückner R, Maurer P, Hakenbeck R.Genome Announc. 2017 May 18;5(20). pii: e00401-17. doi: 10.1128/genomeA.00401-17. PMID: 28522729 </br>2:SU-E-T-226: Clinical Implementation of a Gravity-Oriented Wedge for Total Body Irradiation. Koch N, Yount C, Prado K, Nelson S, Jenrette J, Vanek K.Med Phys. 2012 Jun;39(6Part13):3755. doi: 10.1118/1.4735289. PMID: 28517304 </br>3:Prognostic significance of subclassification of stage IIB lung cancer: A retrospective study of 226 patients. Yin N, Ha M, Liu Y, Gu H, Zhang Z, Liu W.Oncotarget. 2017 Apr 25. doi: 10.18632/oncotarget.17405. [Epub ahead of print] PMID: 28501856 Free Article</br>4:Erratum to /’Air Medical Evacuations From the German North Sea Wind Farm Bard Offshore 1: Traumatic Injuries, Acute Diseases, and Rescue Process Times (2011-2013)/’ [Air Medical Journal 35 (2016) 216-226]. [No authors listed]Air Med J. 2017 May – Jun;36(3):142. doi: 10.1016/j.amj.2016.12.008. Epub 2017 Mar 31. No abstract available. PMID: 28499687 </br>5:Influence of chronic low-dose/dose-rate high-LET irradiation from radium-226 in a human colorectal carcinoma cell line. Vo NTK, Sokeechand BSH, Seymour CB, Mothersill CE.Environ Res. 2017 May 3;156:697-704. doi: 10.1016/j.envres.2017.04.041. [Epub ahead of print] PMID: 28477580 </br>6:Corrigendum to /Eplerenone promotes alternative activation in human monocyte-derived macrophages/ [Pharmacol. Rep. 65 (2013) 226-234]. Łabuzek K, Liber S, Bułdak Ł, Machnik G, Liber J, Okopień B.Pharmacol Rep. 2017 Jun;69(3):592. doi: 10.1016/j.pharep.2017.02.008. Epub 2017 Mar 30. No abstract available. PMID: 28365258 </br>7:Corrigendum to /’specific changes in the proteomic pattern produced by the BRCA1-Ser1841Asn missense mutation/’ [International Journal of Biochemistry and Cell Biology (2007) 220-226]. Crugliano T, Quaresima B, Gaspari M, Faniello MC, Romeo F, Baudi F, Cuda G, Costanzo F, Venuta S.Int J Biochem Cell Biol. 2017 Mar 25. pii: S1357-2725(17)30058-4. doi: 10.1016/j.biocel.2017.03.006. [Epub ahead of print] No abstract available. PMID: 28351545 </br>8:Corrigendum to /p62 modulates the intrinsic signaling of UVB-induced apoptosis/ [Journal of Dermatological Science 83 (2016) 226-233]. Ito S, Kimura S, Warabi E, Kawachi Y, Yamatoji M, Uchida F, Ishibashi-Kanno N, Yamagata K, Hasegawa S, Shoda J, Tabuchi K, Sakai S, Bukawa H, Sekido M, Yanagawa T.J Dermatol Sci. 2017 Jun;86(3):259-260. doi: 10.1016/j.jdermsci.2017.02.284. Epub 2017 Mar 25. No abstract available. PMID: 28351505 </br>9:Corrigendum to /A split G-quadruplex-based DNA nano-tweezers structure as a signal-transducing molecule for the homogeneous detection of specific nucleic acids/ [Biosens. Bioelectron. 74 (2015) 222-226]. Nakatsuka K, Shigeto H, Kuroda A, Funabashi H.Biosens Bioelectron. 2017 Aug 15;94:729. doi: 10.1016/j.bios.2017.03.019. Epub 2017 Mar 11. No abstract available. PMID: 28292558 </br>10:Ra-226 bioaccumulation and growth indices in fish. Shi X, Smith R, Seymour C, Mothersill C.Int J Radiat Biol. 2017 Mar 14:1-10. doi: 10.1080/09553002.2017.1297900. [Epub ahead of print] PMID: 28290238 |
