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Article

Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation.

Blood - 15 Oct 2005

Gotlib Jason, Berubé Caroline, Growney Joseph D, Chen Ching-Cheng, George Tracy I, Williams Christopher, Kajiguchi Tomohiro, Ruan Jia, Lilleberg Stan L, Durocher Jeffrey A, Lichy Jack H, Wang Yanfeng, Cohen Pamela S, Arber Daniel A, Heinrich Michael C, Neckers Len, Galli Stephen J, Gilliland D Gary, Coutré Steven E

Abstract excerpt

The majority of patients with systemic mast cell disease express the imatinib-resistant Asp816Val (D816V) mutation in the KIT receptor tyrosine kinase. Limited treatment options exist for aggressive systemic mastocytosis (ASM) and mast cell leukemia (MCL). We evaluated whether PKC412, a small-molecule inhibitor of KIT with a different chemical structure from imatinib, may have therapeutic use in advanced SM with...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

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Identifiers

PMID: 15972446
DOI: 10.1182/blood-2005-04-1568
PMCID: PMC1895309

Genes

KIT

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

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Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation.PMID 15972446Read ↗

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.Semantic proximity Read ↗

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Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412.Semantic proximity Read ↗

Tyrosine Kinase Inhibition in Mastocytosis: KIT and Beyond KIT.Semantic proximity Read ↗

Mast cell leukemia: identification of a new c-Kit mutation, dup(501-502), and response to masitinib, a c-Kit tyrosine kinase inhibitor.Semantic proximity Read ↗

Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis.Semantic proximity Read ↗

The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic cell types in advanced mastocytosis.Semantic proximity Read ↗

Novel thiazole amine class tyrosine kinase inhibitors induce apoptosis in human mast cells expressing D816V KIT mutation.Semantic proximity Read ↗

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On the way to targeted therapy of mast cell neoplasms: identification of molecular targets in neoplastic mast cells and evaluation of arising treatment concepts.Semantic proximity Read ↗

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