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NVP-TAE 226

Catalog No. T1918 CAS 761437-28-9

Synonyms: TAE226

NVP-TAE 226 (TAE226) is an effective FAK inhibitor (IC50: 5.5 nM) and most effective to Pyk2(IC50: 3.5 nM); 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

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NVP-TAE 226, CAS 761437-28-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 57.00
5 mg	In stock	$ 103.00
10 mg	In stock	$ 166.00
25 mg	In stock	$ 277.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 597.00
1 mL * 10 mM (in DMSO)	In stock	$ 103.00

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Purity: 99.17%

Purity: 98.07%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	NVP-TAE 226 (TAE226) is an effective FAK inhibitor (IC50: 5.5 nM) and most effective to Pyk2(IC50: 3.5 nM); 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.
Targets&IC50	FAK:5.5 nM, PYK2:3.5 nM
In vitro	In in vivo models, NVP-TAE226 (100 mg/kg, p.o.) significantly hindered the growth of human pancreatic tumor MIA PaCa-2 without affecting body weight. Moreover, NVP-TAE226 demonstrated a dose-dependent inhibition of growth and lung metastasis in 4T1 murine mammary tumors, correlated with the suppression of FAK autophosphorylation on Y397 and Akt phosphorylation on serine 473. At a dosage of 75 mg/kg, NVP-TAE226 significantly increased the survival rate of mice bearing intracranial glioma xenografts. Additionally, in a human colorectal cancer SCID mouse model, NVP-TAE226 (100 mg/kg, p.o.) markedly reduced microvessel density.
In vivo	NVP-TAE226 (0.1-10 μM) inhibits microtubule formation in HMEC1 cells and suppresses serum starvation-induced autophosphorylation of FAK(Tyr397) in U87 cells at concentrations below 1 μM. It also inhibits IGF-I-induced phosphorylation of IGF-1R and its downstream target gene activities, including MAPK and Akt in U87 and U251 cells at concentrations under 1 μM. Moreover, NVP-TAE226 at 1 μM inhibits tumor cell invasion by more than 50% in vitro assays on an artificial basement membrane for glioblastoma cell lines. It induces G(2)-M phase arrest in glioblastoma cell lines, including those with wild-type p53, while those bearing mutant p53 undertake apoptosis, evidenced by the activation of caspase-3/7, poly(ADP-ribose) polymerase cleavage, and annexin V apoptosis assays. In the neuroblastoma cell line SK-N-AS, NVP-TAE226 at 5 μM inhibits FAK phosphorylation and at concentrations below 10 μM decreases cell viability, induces cell cycle arrest, and increases apoptosis. In U87 and U251 cells, it impedes tumor cell growth and weakens the G(2)-M cell cycle process related to reduced expression of cyclin B1 and phosphorylated cdc2(Tyr15) proteins at concentrations below 10 μM.
Kinase Assay	Kinase assay: Kinase activities are assayed in Buffer A or C at 30°C, at a final ATP concentration of 15 μM. Blank values are subtracted and activities calculated as pmoles of phosphate incorporated during a 10 min incubation. Controls are performed with appropriate dilutions of dimethylsulfoxide. In a few cases phosphorylation of the substrate is assessed by autoradiography after SDS-PAGE. GSK-3α/β is purified from porcine brain by affinity chromatography on immobilized axin. It is assayed, following a 1/100 dilution in 1 mg BSA/ml 10 mM DTT, with 5 μl 40 μM GS-1 peptide, a specific GSK-3 substrate, (YRRAAVPPSPSLSRHSSPHQSpEDEEE), in buffer A, in the presence of 15 μM [γ-32P] ATP (3,000 Ci/mmol; 1 mCi/ml) in a final volume of 30 μl. After 30 min incubation at 30°C, 25 μl aliquots of supernatant are spotted onto 2.5 × 3 cm pieces of Whatman P81 phosphocellulose paper, and 20 seconds later, the filters are washed five times (for at least 5 min each time) in a solution of 10 ml phosphoric acid/liter of water. The wet filters are counted in the presence of 1 ml ACS scintillation fluid.
Cell Research	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)

Synonyms	TAE226
Molecular Weight	468.94
Formula	C23H25ClN6O3
CAS No.	761437-28-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 87 mg/mL (185.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Liu TJ, et al. Mol Cancer Ther, 2007, 6(4), 1357-1367. 2. Beierle EA, et al. Cancer Invest, 2008, 26(2), 145-151. 3. Schultze A, et al. Invest New Drugs, 2010, 28(6), 825-833. 4. Su Y, Li R, Ning X, et al. Discovery of 2, 4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities[J]. European Journal of Medicinal Chemistry. 2019 May 18;177:32-46.

Citations

1. Sang M, Luo R, Bai Y, et al. BHQ-Cyanine-Based “Off–On” Long-Circulating Assembly as a Ferroptosis Amplifier for Cancer Treatment: A Lipid-Peroxidation Burst Device. ACS Applied Materials & Interfaces. 2019, 11(46): 42873-42884 2. Zheng Q, Zou Y, Teng P, et al. Mechanosensitive Channel PIEZO1 Senses Shear Force to Induce KLF2/4 Expression via CaMKII/MEKK3/ERK5 Axis in Endothelial Cells. Cells. 2022, 11(14): 2191 3. Su Y, Li R, Ning X, et al. Discovery of 2, 4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities. European Journal of Medicinal Chemistry. 2019 May 18;177:32-46 4. Li R, Gong L, Sun J, et al.Discovery of 2, 4-diarylaminopyrimidine derivatives bearing sulfonamide moiety as novel FAK inhibitors.Bioorganic Chemistry.2024: 107134.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library Bioactive Compounds Library Max Angiogenesis related Compound Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library Cytokine Inhibitor Library Anti-Lung Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

NVP-TAE 226 761437-28-9 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK c-Met/HGFR PYK2 IGF-1R inhibit TAE 226 TAE-226 Focal adhesion kinase Insulin Receptor TAE226 NVP-TAE-226 Inhibitor NVP-TAE226 PTK2 protein tyrosine kinase 2 Pyk2 NVPTAE 226 Proline-rich tyrosine kinase 2 NVP TAE 226 PTK2 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.