Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis
Excerpt:
Significantly, dasatinib inhibits the kinase activity of KITD816V with comparable efficiency to wild-type KIT (IC50 of 37 and 79 nM, respectively) in in vitro kinase experiments, whereas the ability of imatinib to inhibit KITD816V kinase activity is highly impaired.