Dasatinib – Broad-Spectrum Tyrosine Kinase Inhibitor
Applications
- Used as a protein kinase inhibitor to study:
- Macrophage polarization and lipogenesis
- Progression of diet-induced steatohepatitis (NASH) and liver fibrosis in mice
- Applied as an SRC tyrosine kinase inhibitor in hepatocellular carcinoma cell studies
- Used to explore autophagy in neuronal cells as a general tyrosine kinase inhibitor
Biochemical / Physiological Actions
Dasatinib is a thiazole-carboxamide compound that inhibits a broad spectrum of protein kinases, including:
- Bcr-Abl (Breakpoint cluster region–tyrosine protein kinase ABL)
- Btk family members
- PDGFR-α/β (Platelet-derived growth factor receptor α/β)
- Ephrin receptor kinases
- Src-family kinases including SRC and LCK
In hematopoietic systems, Dasatinib has been shown to:
- Suppress natural killer (NK) cell cytotoxicity
- Inhibit T lymphocyte activation and proliferation
- Influence platelet activation
It is under active investigation for the treatment of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL).