Tag: VEGFR2

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...

GW806742X, an ATP mimetic, is a Potent MLKL and VEGFR2 Inhibitor

The pseudokinase Mixed Lineage Kinase domain-like (MLKL) is an essential effector protein in the necroptotic cell death pathway downstream of the protein kinase Receptor Interacting Protein Kinase-3 (RIPK3).  RIPK3–mediated phosphorylation of the activation loop in MLKL trips a molecular switch to induce necroptotic cell death. The structure of mouse MLKL...

PF 477736 is a Selective and ATP-Competitive Inhibitor of Chk1

Cancer is a multiplicity of diseases characterized by a range of molecular defects leading to unregulated, aberrant cell growth. Checkpoints are present in all phases of the cell cycle. Checkpoints act as gatekeepers maintaining the integrity of the genome. Researchers use anti-tumor agents to treat cancer by imparting damage...