Remarks: Phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT.
The stem cell factor (SCF) receptor, KIT, also called CD117 or c-KIT receptor, is a member of the type III receptor protein-tyrosine kinase family (RTK). KIT regulate erythropoiesis, lymphopoiesis, megakaryopoiesis, gametogenesis, melanogenesis, with SCF also serving as an important growth factor. gain-of-function mutations in KIT, that is mutations that cause constitutive activation of the tyrosine kinase (TK), have been implicated in a variety of neoplasms including, gastrointestinal stromal tumours (GIST), mastocytosis, acute leukaemias, melanomas and other cancers.In Ba/F3 cells expressing human wildtype KIT, masitinib dose-dependently inhibited SCF-induced cell proliferation with an IC50 of 150 nM.
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