Tag: Flt3

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...

Barasertib, a Pro-Drug of Barasertib-hQPA, is a Highly Selective Aurora B Inhibitor

Aurora kinases play an important role during mitosis for chromosome alignment, segregation, and cytokinesis. Selective Targeting of Aurora B kinase may be a promising therapeutic approach for the treatment of a range of malignancies. In this study, researchers explored the effect of Barasertib. In particular, Barasertib is a highly...

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...

LBW242 is a Potent and Orally Active Proapoptotic IAP Inhibitor

Acute myelogenous leukemia (AML) is a hematologic malignancy. The characteristics include a block in cellular differentiation and aberrant growth of myeloid precursor cells. Approximately 30% of AML patients and a portion of acute lymphoblastic leukemia (ALL) patients express a mutated form of the class III receptor tyrosine kinase, FLT3....

TL02-59 is a Selective and Orally Active Myeloid Src-family Kinase Fgr Inhibitor

Acute myelogenous leukemia (AML) is a devastating hematologic cancer with limited treatments. Scientists have demonstrated that diverse genetic changes are associated with AML. Especially, the upregulation of tyrosine kinase signaling pathways stands for a common feature. Additionally, mutations in the Flt3 receptor tyrosine kinase accounts for almost one-third of...