Tag: Flt3

Dovitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Tyrosine kinase is an enzyme that can transfer phosphate groups from ATP to tyrosine residues of specific proteins in cells. Specifically, this covalent post-translational modification is a key component of normal cell communication and homeostasis maintenance. Tyrosine kinase is an important mediator of signal cascade reaction. Besides, it plays...

Quizartinib (AC220) is an Orally Active and Highly Selective FLT3 Tyrosine Kinase Inhibitor

Receptor tyrosine kinase FMS like tyrosine kinase 3 (FLT3) is a member of the class III receptor tyrosine kinase family. The family also includes FMS, kit, and platelet-derived growth factor (PDGF) receptors. Specifically, FLT3 is relevant to regulating the survival, proliferation, and differentiation of hematopoietic stem/progenitor cells. The normal...

Sorafenib (Bay 43-9006) is an Orally Active Raf Inhibitor

The Raf family consists of three members: A-Raf, B-Raf, and Raf-1. Ras/RAF/MEK extracellular signal-regulated kinase (ERK) pathway is relevant to the control of many basic cellular processes, including proliferation, survival, and differentiation. Specifically, Raf-1 and B-Raf can form heterodimers, which may be important for cell transformation. RAF protein is...

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...

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...