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    TAE226 (NVP-TAE226)
    TAE226 (NVP-TAE226)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0659
    CAS #: 761437-28-9Purity ≥98%

    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 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). 

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

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    Molecular Weight (MW)468.94
    FormulaC23H25ClN6O3
    CAS No.761437-28-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 94 mg/mL (200.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)0.5% methylcellulose: 30 mg/mL
    SynonymsTAE-226, TAE226, TAE 226, NVP-TAE226, NVPTAE226, NVP TAE226,  

    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



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    In Vitro

    In vitro activity: NVP-TAE226 (< 1 μM) inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr397) in serum-starved U87 cells. NVP-TAE226 (< 1 μM) also inhibits IGF-I-induced phosphorylation of IGF-1R and activity of its downstream target genes such as MAPK and Akt in both U87 and U251 cells. NVP-TAE226 (<10 μM) retards tumor cell growth and attenuats G(2)-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr15) protein expression in both U87 and U251 cells. NVP-TAE226 (1 μM) inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay in glioma cell lines. NVP-TAE226 (1 μM) treatment of glioma cell lines containing wild-type p53 mainly exhibits G(2)-M arrest, whereas glioma cell lines bearing mutant p53 undergoes apoptosis, as evidence by detection of caspase-3/7 activation and poly(ADP-ribose) polymerase cleavage and by an Annexin V apoptosis assay. NVP-TAE226 (5 μM) inhibits phosphorylation of FAK in the human neuroblastoma cell line SK-N-AS. NVP-TAE226 (<10 μM) treatment of the human neuroblastoma cell line SK-N-AS leads to decrease in cellular viability, cell cycle arrest, and an increase in apoptosis. NVP-TAE226 (0.1 μM-10 μM) inhibits tube formation of HMEC1 cells.


    Kinase Assay: NVP-TAE 226 is a dual tyrosine kinase inhibitor of FAK (IC50=5.5 nM) and IGF-IR (mean IC50=0.14 μM).


    Cell Assay: Cell cultures are harvested with 0.05% trypsin and seeded in triplicate at 2 × 104 in 24-well culture plates for 24 h before drug treatment. Culture medium is used for mock treatment. Cells (U87 and U251 cell lines) are harvested at the indicated day after treatment, and viable cells are counted using the Vi-cell viability analyze.

    In VivoNVP-TAE226 (75 mg/kg) significantly increases the survival rate of mice bearing intracranial glioma xenografts. NVP-TAE226 (100 mg/kg, oral) exerts significant decrease in microvessel density in a human colon cancer model in SCID mice. NVP-TAE226 (100 mg/kg, oral) efficiently inhibits MIA PaCa-2 human pancreatic tumor growth without body weight loss in vivo model. NVP-TAE226 inhibits 4T1 murine breast tumor growth and metastasis to the lung in a dose-dependent manner in vivo model, associated with inhibition of FAK autophosphorylation at Y397 and Akt phosphorylation at Serine473.
    Animal modelNude mice (male) bearing intracranial glioma xenografts
    Formulation & DosageDissolved in 0.5% methylcellulose; 75 mg/kg; Oral gavage
    ReferencesMol Cancer Ther. 2007 Apr;6(4):1357-67; Invest New Drugs. 2010 Dec;28(6):825-33. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    TAE226 (NVP-TAE226)

    TAE226 treatment inhibits FAK and IGF-IR signaling pathways. Mol Cancer Ther.2007 Apr;6(4):1357-67. 

    TAE226 (NVP-TAE226)

    TAE226 treatment induces apoptosis in glioma cells containing mutant p53. Mol Cancer Ther. 2007 Apr;6(4):1357-67.

    TAE226 (NVP-TAE226)

    TAE226 treatment prolongs the survival of glioma xenograft animals. Mol Cancer Ther. 2007 Apr;6(4):1357-67.


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