TAE226 (NVP-TAE226)

Catalog No.S2820

TAE226 (NVP-TAE226) Chemical Structure

Molecular Weight(MW): 468.94

TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 270 In stock
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2 Customer Reviews

  • Targeting the actin cytoskeleton overcomes resistance to HDACi in primary MM. Graphs representing the proportion of cell death induced in MM patients (n=6) treated LBH589 (5 nM), TAE226 (0.5 uM) and combination.

    Cell Death Dis 2014 5, e1134. TAE226 (NVP-TAE226) purchased from Selleck.

    Role of Tyr397-FAK phosphorylation on HCT-116 cell adhesion and migration. A) Real time adhesion assay and B) Real time migration assay in the presence of P(Tyr397)-FAK inhibitor. HCT-116 cells were treated with the P(Tyr397)-FAK inhibitor NPV-TAE226 at 0.1, 1 and 10 μM for 24 h at 37 °C, 5% CO2, and then seeded on a xCELLigence Roche 16-well plate after it had been functionalized with fibronectin. Cell adhesion and cell migration were monitored for 4 h and 24 h respectively. Each condition was analysed in quadruplicate and the experiment repeated two times.

    J Inorg Biochem, 2016, 160:225-35. TAE226 (NVP-TAE226) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.
PYK2 [1]
(cell-free assay)
FAK [1]
(cell-free assay)
Insulin Receptor [1]
(cell-free assay)
IGF-1R [1]
(cell-free assay)
c-Met [1]
(cell-free assay)
3.5 nM 5.5 nM 43.5 nM 140 nM 160 nM
In vitro

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. [1] 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. [2] NVP-TAE226 (0.1 μM-10 μM) inhibits tube formation of HMEC1 cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cells M2e2V3Bzd2yrZnXyZZRqd25iYYPzZZk> NH\oU401QCCq NGCzSWpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC0PEBpenNiYomgW3NVNTFiYYPzZZktKEmFNUC9NE41KM7:TR?= NITCV3EzPTF6ME[1OC=>
HUVEC MmCySpVv[3Srb36gZZN{[Xl? NXvG[GRVPzJiaB?= MVXBcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCrbjDIWXZGSyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKF[HR1[td5RqdXWuYYTl[EBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OD1zIN88US=> NFXrPW4zOzh2NUKxOy=>
U87MG cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 M1i5b|Q5KGh? MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV6N13HJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OD1zLkKg{txO NVX6TZhpOjVzOEC2OVQ>
PC3 cells NVrNNI41WHKxbHnm[ZJifGmxbjDhd5NigQ>? NEfSNZo1QCCq NWPE[og2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGfTWE0yKGG|c3H5MEBKSzVyPUGuOkDPxE1? NGO4UWYzPTF6ME[1OC=>
MDA-MB-231 cells NVXvTGl7WHKxbHnm[ZJifGmxbjDhd5NigQ>? MmfpOFghcA>? M4DRfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkA1QCCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVA:Oi56IN88US=> MoS5NlUyQDB4NUS=
BT474 cells NIGzWVZHfW6ldHnvckBie3OjeR?= NYTTXFE1OSEQvF2= M17tWlI1KGh? MoLpTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCEVES3OEBk\WyuczDhd5Nme3OnZDDhd{BkdGWjdnHn[UBw\iB6OTDrSIEhWEGUUDDheEAyKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5o M4DYUVE5QTh7OUWw

... Click to View More Cell Line Experimental Data

In vivo NVP-TAE226 (75 mg/kg) significantly increases the survival rate of mice bearing intracranial glioma xenografts. [1] NVP-TAE226 (100 mg/kg, oral) exerts significant decrease in microvessel density in a human colon cancer model in SCID mice. [3] NVP-TAE226 (100 mg/kg, oral) efficiently inhibits MIA PaCa-2 human pancreatic tumor growth without body weight loss in vivo model. [4] 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. [5]


Cell Research:[1]
+ Expand
  • Cell lines: U87 and U251 cell lines
  • Concentrations: 10 μM
  • Incubation Time: 5 days
  • Method: 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 analyze
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Male nude mice bearing intracranial glioma xenografts
  • Formulation: 0.5% methylcellulose
  • Dosages: 75 mg/kg
  • Administration: Administered via oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (200.45 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
0.5% methylcellulose
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 468.94


CAS No. 761437-28-9
Storage powder
Synonyms N/A

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FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID