1. Protein Tyrosine Kinase/RTK
  2. FAK
    Pyk2

NVP-TAE 226 (Synonyms: TAE226)

Cat. No.: HY-13203 Purity: 98.98%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
NVP-TAE 226 Chemical Structure

NVP-TAE 226 Chemical Structure

CAS No. : 761437-28-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $133 In-stock
5 mg $121 In-stock
10 mg $180 In-stock
50 mg $680 In-stock
100 mg $1180 In-stock
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500 mg   Get quote  

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Customer Review

    NVP-TAE 226 purchased from MCE. Usage Cited in: Patent. US 20150175695 A1.

    The small molecule inhibitor for FAK, TAE226, reduces FAK activation and stretch-induced MMP-10 and MMP-12 expression in cultured podocytes. A) Podocytes are cultured on placental laminin in the presence or absence of TAE226 overnight. Extracts are prepared and analyzed by western blot for expression of pFAK397 and total FAK. FAK activation is also analyzed by western blot of podocyte extracts from stretched and non-stretched cells, demonstrating that biomechanical stretching directly activates

    NVP-TAE 226 purchased from MCE. Usage Cited in: Patent. US 20170285005 A1.

    TAE226 reduces FAK activation and stretch-induced MMP-10 and MMP-12 expression in cultured podocytes.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    IC50: 5.5 nM (FAK), 3.5 nM (Pyk2), 0.14 μM (IGF-IR), 0.16 μM (c-Met), 0.36 μM (KDR), 0.48 μM (Flt3)[1]

    In Vitro

    NVP-TAE 226 (TAE226), a potent ATP-competitive inhibitor of several tyrosine protein kinases, in particular FAK and IGF-IR kinases. In a cell-based kinase assays, FAK, IGF-IR kinase, and IR kinase are inhibited with an IC50 range of 100 to 300 nM compared with the other kinases tested, which are >10-fold less sensitive. In culture, NVP-TAE 226 inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr395). NVP-TAE 226 also inhibits IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. NVP-TAE 226 retards tumor cell growth as assessed by a cell viability assay and attenuates G2-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr15) protein expression. NVP-TAE 226 treatment inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay. Interestingly, TAE226 treatment of tumor cells containing wild-type p53 mainly exhibits G2-M arrest, whereas tumor cells bearing mutant p53 underwent apoptosis[1].

    In Vivo

    Treatment with NVP-TAE 226 (TAE226) at 50 or 75 mg/kg extends the median survival of U87 xenograft animals by 6 and 7 days, respectively (P=0.084 and P=0.042, respectively, compared with vehicle-treated animals). However, NVP-TAE 226 treatment of LN229-engrafted animals significantly prolongs their median survival by 19 days (P<0.004 for both dosages, compared with vehicle-treated animals)[1].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.1325 mL 10.6623 mL 21.3247 mL
    5 mM 0.4265 mL 2.1325 mL 4.2649 mL
    10 mM 0.2132 mL 1.0662 mL 2.1325 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    NVP-TAE 226 (TAE226) is dissolved in DMSO (10 mM) and stored (−20°C), and then diluted with DMEM (DMSO ≤0.1%) before use[1].

    Glioma 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 are harvested at the indicated day after treatment, and viable cells are counted using the Vi-cell viability analyzer. The antiproliferative activity of NVP-TAE 226 (ranging from 0.25 to 1 μM) on cells growing in culture is determined using a tetrazolium-based colorimetric MTT assay[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    NVP-TAE 226 (TAE226) is prepared in 0.5% methylcellulose[1].

    Mice[1]
    Male nude mice used for this study are 6 to 8 weeks old. In DMEM/F12 serum-free media (5 μL), 5×105 of U87 cells and 1×106 of LN229 cells per mouse are implanted intracranially through a guide-screw system. Four days after injection of the tumor cells, mice are randomized into three groups for each cell line (n=6). Mice in group 1 are treated with 50 mg/kg NVP-TAE 226 in 200 μL of 0.5% methylcellulose, via an oral gavage. The mice in group 2 receive 75 mg/kg NVP-TAE 226 in 200 μL of 0.5% methylcellulose. The mice in group 3 the same vehicle used for administration of NVP-TAE 226 (control). Treatment frequency is once a day for 5 days and off for 2 days, for a duration of 4 weeks. Mice are monitored daily. Mice are euthanized when they are moribund, and the whole brain is extracted for rapid freezing in liquid nitrogen and storage at -70°C. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    468.94

    Formula

    C₂₃H₂₅ClN₆O₃

    CAS No.

    761437-28-9

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    NVP-TAE 226 (TAE226) is diluted in a 0.5% carboxymethylcellulose suspension[2].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    NVP-TAE 226
    Cat. No.:
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