Tag: Tyrosine Kinase

Lapatinib is a Potent Inhibitor of the ErbB-2 and EGFR Tyrosine Kinase Domains

Growth factors and their transmembrane receptor tyrosine kinase play important roles in cell proliferation, survival, migration, and differentiation. Additionally, Epidermal growth factor (EGF)-like proteins stimulates cells to divide by activating members of the EGF receptor (EGFR) family. Many types of human tumor cells growth and development are related to the...

Tivantinib is a Selective c-Met Tyrosine Kinase Inhibitor

c-Met (hepatocyte growth factor receptor, HGFR) is a type of receptor tyrosine kinase which belongs to the MET family.  c-Met exsists in the surfaces of various epithelial cells. Hepatocyte growth factor (HGF) is the ligand for c-Met. HGF belongs to the soluble cytokine family and is also a member...

Quizartinib (AC220) is an Orally Active and Highly Selective FLT3 Tyrosine Kinase Inhibitor

Receptor tyrosine kinase FMS like tyrosine kinase 3 (FLT3) is a member of the class III receptor tyrosine kinase family. The family also includes FMS, kit, and platelet-derived growth factor (PDGF) receptors. Specifically, FLT3 is relevant to regulating the survival, proliferation, and differentiation of hematopoietic stem/progenitor cells. The normal...

TL02-59 is a Selective and Orally Active Myeloid Src-family Kinase Fgr Inhibitor

Acute myelogenous leukemia (AML) is a devastating hematologic cancer with limited treatments. Scientists have demonstrated that diverse genetic changes are associated with AML. Especially, the upregulation of tyrosine kinase signaling pathways stands for a common feature. Additionally, mutations in the Flt3 receptor tyrosine kinase accounts for almost one-third of...

Multiple Tyrosine Kinases Inhibitor TAS-115

VEGF signaling via VEGF receptor is a pivotal factor for tumor angiogenesis that regulates tumor progression. However, VEGFR-targeted inhibitor monotherapies showed limited effects on various carcinomas. And even combination therapies with chemotherapeutic agents are unsatisfactory. MET is a receptor for HGF. The HGF-MET signaling also participated in regulating tumor progression,...

AZD3229 is a Potent Pan-KIT Mutant Inhibitor

Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal neoplasms of the gastrointestinal tract. While the application of targeted tyrosine kinase inhibitors has revolutionized the treatment of gastrointestinal stromal tumors (GISTs). The targeted tyrosine kinase inhibitors inhibit KIT-driven proliferation, diverse mutations to this kinase drive resistance to established therapies....