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CAS No. 761437-28-9
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. TAE226 (NVP-TAE226) induces apoptosis.
Selleck's TAE226 (NVP-TAE226) has been cited by 18 publications
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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.
The numbers of BrdU-positive cells were significantly increased by pre-treatment of NGF in SVZ and SGZ. Compared with the IgG group (a1 and a2), the numbers of BrdU-positive cells were significantly higher in the NGF group (b1 and b2). Compared with the NGF group, the numbers of BrdU-positive cells were significantly lower than in the TAE226 groups (c1 and c2) (n=3/group; *P < 0.01; **P < 0.05; 200×).
Neurosci Lett, 2018, 672:96-102. TAE226 (NVP-TAE226) purchased from Selleck.
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|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. TAE226 (NVP-TAE226) induces apoptosis.|
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. 
|In vivo||NVP-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. |
-  Liu TJ, et al. Mol Cancer Ther, 2007, 6(4), 1357-1367.
-  Beierle EA, et al. Cancer Invest, 2008, 26(2), 145-151.
-  Schultze A, et al. Invest New Drugs, 2010, 28(6), 825-833.
|In vitro||DMSO||94 mg/mL (200.45 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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