Sitravatinib (MGCD516) is an Orally Bioavailable RTK Inhibitor with PD-1 Blockade Activity
Sarcomas are rare but highly aggressive mesenchymal tumors. Mutation and overexpression of many receptor tyrosine kinases (RTKs) including c-Met, PDGFR, c-Kit and IGF1-R drive defective signaling pathways in sarcomas. Sitravatinib is a small molecule inhibitor targeting multiple receptor tyrosine kinases involved in driving sarcoma cell growth. Moreover, Sitravatinib significantly...
IACS-13909 is a Selective and Orally Active SHP2 Inhibitor
Src homology 2 domain-containing phosphatase (SHP2) is a phosphatase that mediates signaling downstream of multiple receptor tyrosine kinases. SHP2 suppresses signaling through the MAPK pathway. Furthermore, SHP2 inhibition has demonstrated tumor growth inhibition in receptor tyrosine kinases-activated cancers. In this study, researchers report the discovery of IACS-13909. IACS-13909 is...
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...