Telatinib is an Orally Active Inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit
The importance of angiogenesis in solid tumor growth is well established. Inhibition of the vascular endothelial growth factor (VEGF)/VEGF receptor (VEGFR) pathway is now an approved and generally accepted treatment of lung cancer. Interestingly, bevacizumab, a monoclonal antibody against VEGF-A, is predominantly administered in combination with chemotherapy, whereas the...
Axitinib is a Multi-Targeted Tyrosine Kinase Inhibitor
Vascular endothelial growth factor (VEGF) is an important signal protein. Importantly, it is involved in angiogenesis and angiogenesis (blood vessels grow from a pre-existing vascular system). All members of VEGF family stimulate cell response by binding to tyrosine kinase receptors (VEGFRs) on the cell surface. Thus they dimerize and...
Sorafenib (Bay 43-9006) is an Orally Active Raf Inhibitor
The Raf family consists of three members: A-Raf, B-Raf, and Raf-1. Ras/RAF/MEK extracellular signal-regulated kinase (ERK) pathway is relevant to the control of many basic cellular processes, including proliferation, survival, and differentiation. Specifically, Raf-1 and B-Raf can form heterodimers, which may be important for cell transformation. RAF protein is...
Sitravatinib (MGCD516) is an Orally Bioavailable RTK Inhibitor with PD-1 Blockade Activity
Sarcomas are rare but highly aggressive mesenchymal tumors. Mutation and overexpression of many receptor tyrosine kinases (RTKs) including c-Met, PDGFR, c-Kit and IGF1-R drive defective signaling pathways in sarcomas. Sitravatinib is a small molecule inhibitor targeting multiple receptor tyrosine kinases involved in driving sarcoma cell growth. Moreover, Sitravatinib significantly...