Tag: c-Met

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...

XL092 is a Potent Axl, Mer and C-Met kinase Inhibitor

Human Axl belongs to the TAM subfamily of receptor tyrosine kinases that includes Mer. TAM kinases contain two immunoglobulin-like domains and two fibronectin type III domains. Many cancer cells exhibit overexpressed Axl. And it is initially cloned from patients with chronic myelogenous leukemia. Axl has been associated with cancers...

Crizotinib is an Orally Active, ATP-Competitive ALK and c-Met inhibitor

In this article, we will introduce an orally bioavailable, ATP-competitive ALK and c-Met inhibitor, Crizotinib. The IC50 values for ALK and c-Met kinases are 20 and 8 nM, respectively. Additionally, in cell-based assays, Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM, respectively. In...

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...

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...

AMG-458 is a Selective and Orally Bioavailable c-Met Inhibitor

C-met is a protein encoded by a met gene in humans, which has tyrosine kinase activity. Specifically, Met is an essential one-way tyrosine kinase receptor for embryonic development, organogenesis, and wound healing. Besides, C-met is a receptor tyrosine kinase that can be activated by its ligand, hepatocyte growth factor/dispersion...

BPI-9016M is an Orally Active and Selective Dual c-Met/AXL Inhibitor

c-Met is a membrane-spanning receptor tyrosine kinase. It has a high affinity for binding to hepatocyte growth factor (HGF). As we all know, HGF/c-Met signaling often involves activation of its downstream pathways. High-level Met gene amplification, mutation or protein overexpression can lead to aberrant activation of the HGF/c-Met pathway. In...