Name: TAE226 (NVP-TAE226)
Price: 277.00 USD

- Overview
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    Background
    
    TAE226 (NVP-TAE226) is a selective inhibitor of FAK with IC50 value of 5.5 nM [1].
    Focal Adhesion Kinase (FAK) also known as PTK2 protein tyrosine kinase 2 (PTK2) is a focal adhesion-associated protein kinase and plays an important role in cellular adhesion and spreading processes [1].
    TAE226 (NVP-TAE226) is a potent FAK inhibitor and has a different selectivity with the reported FAK inhibitor PF-562271. 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 μmol/L) and U87/EGFR, as well as U87/EGFRvIII, which had higher p-FAK expression than U87 were more sensitive to TAE226 (NVP-TAE226). Then, it was shown that TAE226 (NVP-TAE226) treatment inhibited Glioma cell invasion and induced apoptosis when tested with U251 and LN18 cell lines [1]. In the medullary thyroid tumor cell line MZ-CRC-1, TAE226 (NVP-TAE226) (100 nM and 1000 nM) treatment for 72 h inhibited cell proliferation, prolonged cellular processes and decreased cell invasion ability [2].
    In male nude mice model with U87 subcutaneous xenograft, administration of TAE226 (NVP-TAE226) (50 or 75 mg/kg) prolonged the median survival of animals by 7 days with significant difference compared with control group (29 days) [1].
    It is also reported that TAE226 (NVP-TAE226) is a potent inhibitor for Pyk2 with IC50 value of 3.5 nM [1].
    
    [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.
- Properties
  - Alternative Name
    
    TAE 226;TAE-226; 2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]-N-methylbenzamide
    
    CAS Number
    
    761437-28-9
    
    Molecular Formula
    
    C23H25ClN6O3
    
    Molecular Weight
    
    468.94
    
    Appearance
    
    A solid
    
    Purity
    
    98.54%
    
    Solubility
    
    ≥23.45 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Menanteau-Ledouble S, Lawrence ML, et al. "Invasion and replication of Yersinia ruckeri in fish cell cultures." BMC Vet Res. 2018 Mar 9;14(1):81. PMID:29523132

TAE226 (NVP-TAE226)

TAE226 (NVP-TAE226)

Background

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