Dasatinib
Tyrosine kinase inhibitor; Inhibits ABL, SRC, LCK and YES
Dasatinib
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Dasatinib is a potent, ATP-competitive tyrosine kinase inhibitor. It is specific for SRC/ABL kinases, for example, ABL, SRC, LCK, and YES with IC₅₀ values of < 1.0, 0.5, 0.4 and 0.5 nM, respectively, and also demonstrates activity against KIT with an IC₅₀ = 5.0 nM (Lombardo et al.; Davis et al.) Dasatinib is a second-generation inhibitor of the oncogenic tyrosine kinase BCR-ABL with 325-fold more potency than imatinib, and is also able to inhibit imatinib-resistant BCR-ABL mutants (Tokarski et al.). It also inhibits a large number of other kinases (76 of 148 kinases tested) when screened at 10 μM (Carter et al.).
CANCER RESEARCH
- Inhibits proliferation in cell lines derived from chronic myeloid leukemia (CML), prostate, breast, and colon tumors (Lombardo et al.).
- Inhibits proliferation of cells with imatinib-resistant BCR-ABL mutations (Shah et al.).
- Inhibits tumor growth and development of lymph node metastases in orthotopic nude mouse models of prostate cancer (Park et al.).
- Induces cell-cycle arrest and apoptosis and decreases growth in thyroid cancer cells (Chan et al.).
- Inhibits production of extracellular matrix proteins in dermal fibroblasts and prevents development of bleomycin-challenge-induced fibrosis in mice (Distler & Distler; Akhmetshina et al.).
