Vatalanib (PTK787) is an Inhibitor of VEGFR2/KDR
Vascular endothelial growth factor receptor (VEGFR) is the receptor for VEGF. VEGF is an important signaling protein involved in both vasculogenesis and angiogenesis. VEGFRs consist of three subtypes, the fms-like tyrosine kinase Flt-1 (VEGFR1/Flt-1), the kinase domain region, also referred to as fetal liver kinase (VEGFR2/KDR/Flk-1), and Flt-4 (VEGFR3)....
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...
VAL-083 Creates DNA N7 Methylation with Antitumor Activity
Glioblastoma (GBM) is one of the most difficult tumors. Many new agents fail to cross the blood-brain barrier (BBB) and it has intrinsic drug resistance. VAL-083 is an alkylating agent that creates N7 methylation on DNA. Additionally, VAL-083 suppresses U251 and SF188 cell growth and induces apoptosis after 72...
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...
Cabozantinib is a potent Multiple Receptor Tyrosine Kinases (RTKs) Inhibitor
Receptor tyrosine kinases (RTKs) are high-affinity cell surface receptors for many polypeptide growth factors, cytokines, and hormones. Specifically, RTKs are part of a larger family of protein tyrosine kinases. RTKs are key regulators of normal cellular processes. Besides, it plays a key role in the development and progression of...
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...