JBJ-04-125-02 is a Mutant-Selective and Orally Active EGFR Inhibitor
Epidermal growth factor receptor (EGFR) is a transmembrane receptor protein in humans. The discovery of activating mutations in EGFR detected in 10% to 30% of patients with non–small cell lung cancer (NSCLC). In addition, it has revolutionized the treatment of this disease. Until recently, EGFR tyrosine kinase inhibitors (TKI), including...
HKI-357 is an Irreversible Dual Inhibitor of EGFR and ERBB2
Non-small cell lung cancers with activating mutations in the kinase domain of the EGFR demonstrate dramatically, but transient, responses to the reversible tyrosine kinase inhibitors Gefitinib. To identify mechanisms of resistance to Gefitinib, Researchers used NSCLC cells harboring an activating EGFR mutation to generate multiple resistant clones. The bronchoalveolar...
PKI-166 is a Selective and Orally Bioavailable EGFR Autophosphorylation Inhibitor
Human pancreatic cancer cells can secrete the proangiogenic molecules, such as VEGF, IL-8, and basic fibroblast growth factor. VEGF is the major proangiogenic factor in most types of human cancer. Therefore, in this article, we will introduce a potent, selective and orally active EGFR tyrosine kinase inhibitor, PKI-166. Firstly,...
CGP52411 is an Orally Active and ATP-Competitive EGFR Inhibitor
The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein that mediates the response of cells to EGF and transforming growth factor α. Deregulated signal transduction via the EGFR family of protein-tyrosine kinase growth factor receptors is relevant to proliferative diseases. Besides, the EGFR is involved in epithelial proliferation...
BI-4020 is an Orally Active EGFR Tyrosine Kinase Inhibitor
The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase that transduces mitogenic signals. When EGFR carries an activating mutation, it can be an oncogenic driver in lung tumors. Notably, Since additional mutation in the EGFR kinase domain that confers resistance to TKIs, lung cancer patients relapse within...
AG-825, a selective ErbB2 inhibitor with anti-cancer effect
The ErbB tyrosine kinase receptor (RTK) family has 4 members: ErbB1 (EGFR/HER1), ErbB2 (HER2/neu), ErbB3 (HER3), and ErbB4 (HER4). These receptors are cell surface receptors and play important roles in cell proliferation, survival, and growth signaling. ErbB2 is an orphan receptor; it can associate with other ErbBs to enhances...
TX1-85-1, a ATP-competitive ligand of Her3, covalent modification of Her3 to inhibit Her3 signaling
Her3 (also known as ErbB3) is a member of the epidermal growth factor receptor (EGFR) tyrosine kinases, including Her1, Her2 and Her4. However, owing to receptor or ligand overexpression or oncogenic mutations that results in constitutive activation of the kinase domain. EGFR family-dependent signaling frequently becomes deregulated in human...