Tag: RTK

TNO155 is an Orally Active WT SHP2 Inhibitor with Antineoplastic Activity

SHP2 is a non-receptor ubiquitous protein tyrosine phosphatase and has a relatively conserved structure and function. The SHP2 includes the PTP domain, two SH2 domains, and a C-terminal tail containing two phosphorylation sites. Binding of the N-SH2 domain with the PTP domain is able to inhibit SHP2 activity. N-SH2...

BAY-474, a SGC Epigenetic Probe, is a Tyrosine-Protein Kinase c-Met Inhibitor

Potent, selective and broadly characterized small molecule modulators of protein function (chemical probes) are powerful research reagents. Genetic approaches are used to suppress the expression of the respective gene/protein. However, these methods have some deficiencies in drug discovery. They commonly remove or suppress the entire protein and they are...

Ravoxertinib is an Orally Active and Highly Selective ERK1/2 Inhibitor

The RAS/RAF/MEK/ERK (MAPK) signal transduction pathway has attracted significant interest as a therapeutic target for cancer. ERK1/2 phosphorylates more than 50 downstream substrates responsible for cell growth, proliferation, survival, angiogenesis, and differentiation. Small molecule inhibitors of BRAF and MEK have shown promising activities in a variety of solid tumors...