JCN037 is a Non-Covalent and Brain-Penetrant EGFR Inhibitor
The epidermal growth factor receptor (EGFR) is a transmembrane protein that is a receptor for members of the EGF family of extracellular protein ligands. In many cancer types, mutations affecting EGFR expression or activity could result in cancer. Specifically, EGFR gene changes occurred in nearly 60% of glioblastoma tumors....
PD-089828 is an Inhibitor of FGFR-1, PDGFR-β, EGFR and c-Src Tyrosine Kinase
Protein tyrosine kinases comprise a group of enzymes. They catalyze the phosphorylation of certain proteins on specific tyrosine residues. The growth factor receptor tyrosine kinases are a subfamily. The kinases are activated on the high-affinity binding of growth factors to their cognate receptors. Members of this subfamily include PDGFR...
PD-161570 is an Inhibitor of FGF-1R, PDGFR, EGFR and c-Src Tyrosine Kinases
Fibroblast growth factors (FGF) are a family of cell-signaling proteins, which are involved in many processes, especially as the key factor of normal development. In addition, the FGFR family consists of a group of four homologous receptor tyrosine kinases. Besides, FGF1 was a member of a family of FGF...
CGP77675 is an Orally Active Inhibitor of Src Family Kinases
Src kinase family is a nonreceptor tyrosine kinase family. It includs 9 members: SRC, yes, Fyn and FGR, Lck, HCK, BLK, and Lyn. Specifically, Src family kinases interact with many cytoplasmic, nuclear, and membrane proteins and modify these proteins by phosphorylation of tyrosine residues. Besides, tyrosine kinase SRC is...
ONO-7475 is a Selective and Orally Active AXL/Mer Inhibitor
EGFR tyrosine kinase inhibitors (EGFR-TKIs) are efficient for the treatment of non-small cell lung cancer (NSCLC) harboring EGFR mutations. However, most EGFR-positive NSCLC patients exhibit resistance to EGFR-TKIs after sometimes. The 3rd generation EGFR-TKI Osimertinib shows efficacy for overcoming EGFR T790M mutation-positive NSCLC. Anexelekto (AXL) belongs to the TAM...
CCT365623, an Orally Active LOX Inhibitor, Supresses EGFR (pY1068) and AKT Phosphorylation
Lysyl oxidase (LOX) is a copper and quinone-cofactor containing amine oxidase. It is an inactive pro-enzyme and can be cleaved to a mature active form by extracellular metalloproteases. LOX prompts the formation of covalent bonds in collagens and elastin. Thereby, it increases the stiffness of the ECM. Besides, many...
LCH-7749944 is a Potent PAK4 Inhibitor and Induces Apoptosis
P21-activated kinase 4 (PAK4) is a serine/threonine protein kinase and has related to the regulation of cytoskeleton recombine, cell proliferation, gene transcription, carcinogenic transformation, cell invasion. Moreover, PAK4 overexpression, mutations, genetic amplification were detected in a variety of human tumors, making it a potential therapeutic target. Specifically, The p21-activated kinases...