TAE226 (NVP-TAE226)
Catalog No.S2820
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.
Cited by 6 Publications
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2 Customer Reviews
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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
Choose Selective FAK Inhibitors
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. | |||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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] |
Protocol
| Cell Research:[1] |
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| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 94 mg/mL (200.45 mM) |
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| 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 |
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| Formula | C23H25ClN6O3 |
| CAS No. | 761437-28-9 |
| Storage | powder |
| Synonyms | N/A |
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