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....
G5-7, an Orally Active JAK2 Inhibitor, Induces Cell Cycle Arrest and Apoptosis
JAK2 and STAT3 have been extensively implicated in the development and progression of numerous cancers. STAT3 be also activated by EGFR, JAK2, and other TYKs activated by EGF, LIF, and other cytokines. STAT3 constitutively activats in 60% of primary malignant gliomas, and the extent of activation correlates with glioma...
M8891 is an Orally Active and Brain Penetrant MetAP-2 Inhibitor
Removal of N-terminal methionine by methionine aminopeptidases (MetAP) is a crucial step in the maturation of proteins during protein biosynthesis. Besides, MetAP-2 is one of the two cytoplasmic methionine aminopeptidases expressed in mammalian cells. Moreover, MetAP-2 acts as a target of the highly potent and irreversible inhibitor fumagillin to...