Tag: VEGFR

Motesanib is a potent ATP-Competitive Inhibitor of VEGFR1/2/3

There are numerous growth factors involved in tumor angiogenesis, but foremost among them is the family of vascular endothelial growth factors (VEGFs). The VEGF family includes VEGFA, VEGFB, VEGFC, VEGFD, and placenta growth factor (PGF). These ligands bind with different affinities to three endothelial receptor tyrosine kinases (RTKs), such...

Golvatinib (E-7050) is a potent Dual Inhibitor of both c-Met and VEGFR2 Kinases

c-Met is the cellular receptor for the hepatocyte growth factor (HGF). Activation of the HGF⁄c-Met pathway always leads to tumor progression, invasion, and metastasis. Vascular endothelial growth factor (VEGF) is an important molecule in tumor progression. Additionally, VEGF is associated with tumor angiogenesis. Due to their important role in...

CPL304110 is an Orally Active and Selective FGFR(1-3) Inhibitor

Over the last decade, the FGFRs family has become an attractive validated therapeutic target notably in cancer. It consists of four members (FGFR1 to FGFR4) which are structurally related cell surface RTKs. This FGF-FGFR axis participates in key biological processes that play significant roles in cell functions such as...

AZD4547 is a Potent FGFR Family Inhibitor

Fibroblast growth factors (FGF) and their receptors play important roles in multiple biologic processes, such as tissue repair, hematopoiesis, angiogenesis, and embryonic development. The FGFR family mainly comprises 4 main members (FGFR1–4). FGFRs and FGFRs FGF ligand binding can result in FGFR dimerization. In addition, receptor autophosphorylation and activation...

Vorolanib is an Orally Active Inhibitor of VEGFR and PDGFR 

Vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) are cell-surface tyrosine kinase receptors. They represent targets for anticancer therapy in solid tumors. For accurately validating the therapeutic potential of these target-specific agents, the in vivo quantification of VEGFR/PDGFR activity is critically important. It is not...