Tag: VEGFR

Olinvacimab (TTAC-0001) is a Human Anti-VEGFR2 mAb for Cancer Research

Olinvacimab (TTAC-0001) is a fully human anti-VEGFR2 monoclonal antibody from a fully human naive single-chain variable fragment phage library. Olinvacimab (TTAC-0001) inhibits VEGF and binds to KDR with a Kd value of 0.23 nM. Additionally, Olinvacimab (TTAC-0001) (0-1000 nM) inhibits the binding of VEGF to its receptor KDR with...

Dovitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Tyrosine kinase is an enzyme that can transfer phosphate groups from ATP to tyrosine residues of specific proteins in cells. Specifically, this covalent post-translational modification is a key component of normal cell communication and homeostasis maintenance. Tyrosine kinase is an important mediator of signal cascade reaction. Besides, it plays...

Nintedanib is an Orally Active Triple Angiokinase Inhibitor for VEGFR, FGFR and PDGFR

VEGFR are receptors for vascular endothelial growth factor (VEGF). There are three main subtypes: VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, and VEGFR3. VEGFR1 and 2 are expressed on vascular endothelial cells, whereas VEGFR3 is expressed on lymphatic endothelial. VEGFR1 and VEGFR2 play major roles in physiological as well as pathological angiogenesis. VEGFR3 can...

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...