Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants, with the exception of T315I. Dasatinib has a two-log (∼325-fold) increased potency relative to imatinib. Dasatinib is a potent wild-type and mutant c-Abl inhibitor, except T315I. Dasatinib directly targets wild-type and mutant c-Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Dasatinib displays 325-fold greater potency compared with imatinib against cells expressing wild-type Bcr-Abl. Dasatinib treatment inhibits SRC signaling, decreases growth, and induces cell cycle arrest and apoptosis in a subset of thyroid cancer cells. Dasatinib (anhydrous) is an inhibitor of c-Src.
See how others have used Dasatinib. Click on the entry to view the PubMed entry .
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