tae226 has been researched along with Pancreatic-Neoplasms* in 3 studies
3 other study(ies) available for tae226 and Pancreatic-Neoplasms
| Article | Year |
|---|---|
Design, synthesis and activity evaluation of isopropylsulfonyl-substituted 2,4- diarylaminopyrimidine derivatives as FAK inhibitors for the potential treatment of pancreatic cancer.
Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Focal Adhesion Protein-Tyrosine Kinases; Humans; Mice; Pancreatic Neoplasms; Protein Kinase Inhibitors; Pyrimidines | 2022 |
Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines.
A family of phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) were synthesized as potent focal adhesion kinase (FAK) inhibitors. The PA-DPPY derivatives could significantly inhibit the FAK enzymatic activity at concentrations lower than 10.69 nM. Among them, compounds 7a and 7e were two of the most active FAK inhibitors, possessing IC Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dimethoate; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Focal Adhesion Kinase 1; Humans; Molecular Docking Simulation; Molecular Structure; Pancreatic Neoplasms; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship | 2017 |
3D cell cultures of human head and neck squamous cell carcinoma cells are radiosensitized by the focal adhesion kinase inhibitor TAE226.
Focal adhesion kinase (FAK), a main player in integrin signaling and survival, is frequently overexpressed in human cancers and therefore postulated as potential target in cancer therapy. The aim of this study was to evaluate the radiosensitizing potential of the FAK inhibitor TAE226 in three-dimensional (3D) tumor cell cultures.. Head and neck squamous cell carcinoma (HNSCC) cells (FaDu, UT-SCC15, UT-SCC45), lung cancer cells (A549), colorectal carcinoma cells (DLD-1, HCT-116) and pancreatic tumor cells (MiaPaCa2, Panc1) were treated with different concentrations of TAE226 (0-1mum; 1 or 24h) without or in combination with irradiation (0-6Gy, X-ray, single dose). Subsequently, 3D clonogenic survival assays (laminin-rich extracellular matrix) and Western blotting (expression/phosphorylation, e.g. FAK, Akt, ERK1/2) were performed.. All investigated 3D cell cultures showed a dose-dependent reduction in clonogenic survival by TAE226. Intriguingly, TAE226 only significantly radiosensitized 3D HNSCC cell cultures accompanied by a pronounced dephosphorylation of FAK, Akt and ERK1/2.. Our data demonstrate TAE226 as potent FAK inhibitor that enhances the cellular radiosensitivity particularly of HNSCC cells grown in a 3D cell culture model. Future in vitro and in vivo investigations will clarify, to which extent this approach might be clinically relevant for radiotherapy of HNSCC. Topics: Apoptosis; Carcinoma, Squamous Cell; Cell Movement; Cell Proliferation; Cell Survival; Colorectal Neoplasms; Dose-Response Relationship, Drug; Focal Adhesion Protein-Tyrosine Kinases; Head and Neck Neoplasms; Humans; Lung Neoplasms; Morpholines; Pancreatic Neoplasms; Probability; Radiation Tolerance; Radiation, Ionizing; Tumor Cells, Cultured | 2009 |