Category: Gastric Cancer

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...

ABT-737 is a Selective and BH3 Mimetic Bcl-2, Bcl-xL and Bcl-w Inhibitor

Bcl-2 protein family is a key regulator of apoptosis and a marker of B-cell lymphoma. Importantly, apoptosis is an important physiological process of selective cell clearance, involving a variety of biological events. Particularly, the Bcl-2 family is the most characteristic protein family involved in regulating apoptotic cell death. It...

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...

SIS3 is a Potent and Selective Inhibitor of Smad3 Phosphorylation

Smad contains a series of proteins with similar structures, which are the main signal transducer in transforming growth factors β (TGF-b) superfamily. Specifically, they play an important role in the regulation of cell development and growth. One mechanism of Smads promoting TGF-b-induced cell arrest is down-regulation of Myc, a...

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...