Article
PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects.
Blood - 15 Jan 2006
Gleixner Karoline V, Mayerhofer Matthias, Aichberger Karl J, Derdak Sophia, Sonneck Karoline, Böhm Alexandra, Gruze Alexander, Samorapoompichit Puchit, Manley Paul W, Fabbro Doriano, Pickl Winfried F, Sillaber Christian, Valent Peter
Abstract excerpt
In most patients with systemic mastocytosis (SM), including aggressive SM and mast cell leukemia (MCL), neoplastic cells express the oncogenic KIT mutation D816V. KIT D816V is associated with constitutive tyrosine kinase (TK) activity and thus represents an attractive drug target. However, imatinib and most other TK inhibitors fail to block the TK activity of KIT D816V. We show that the novel TK-targeting drugs...
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