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NVP-TAE 226

Catalog No. T1918 CAS 761437-28-9

Synonyms: TAE226

NVP-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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

NVP-TAE 226, CAS 761437-28-9

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Purity: 98%

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Description	NVP-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	PYK2:3.5 nM, FAK:5.5 nM
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 2 years

Solubility Information

DMSO: 87 mg/mL (185.5 mM)

Ethanol: <1 mg/mL

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Preclinical Compound Library Anti-Lung Cancer Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library

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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 蛋白酪氨酸激酶凋亡细胞骨架血管生成 Apoptosis c-Met/HGFR FAK IGF-1R PYK2 inhibit TAE-226 Focal adhesion kinase Insulin Receptor TAE226 Inhibitor PTK2 protein tyrosine kinase 2 Pyk2 NVPTAE 226 Proline-rich tyrosine kinase 2 NVP TAE 226 PTK2 TAE 226 inhibitor

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