Tag: RTK

Toceranib is An Orally Active Inhibitor of Receptor Tyrosine Kinase (RTK)

Toceranib is an orally active receptor tyrosine kinase (RTK) inhibitor. Besides, Toceranib inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. What’s more, Toceranib has antitumor and antiangiogenic activity and has the potential to recurrent, non-resectable grades 2 and 3 canines MCTs....

Axitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Vascular endothelial growth factor (VEGF) is an important signal protein. Importantly, it is involved in angiogenesis and angiogenesis (blood vessels grow from a pre-existing vascular system). All members of VEGF family stimulate cell response by binding to tyrosine kinase receptors (VEGFRs) on the cell surface. Thus they dimerize and...

Ganetespib (STA-9090) is a HSP90 Inhibitor

Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated 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...

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...