Sensitivity of human cells bearing oncogenic mutant kit isoforms to the novel tyrosine kinase inhibitor INNO-406

Jingxuan Pan, Alfonso Quintás-Cardama, Taghi Manshouri, Jorge Cortes, Hagop Kantarjian, Srdan Verstovsek

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15 Scopus citations

Abstract

The activity of the novel tyrosine kinase inhibitor INNO-406 against human cells with mutated KIT was investigated. Human mast cell (HMC)-1.1 cells with juxtamembrane domain mutation V560G, and HMC-1.2 cells with both V560G and the kinase domain mutation D816V, were treated with INNO-406 (0.02-5.00 μM) or imatinib for 72 h. INNO-406 and imatinib were equipotent against HMC-1 cells regarding cell proliferation (IC50 51 nM and 75 nM, respectively), inhibition of KIT phosphorylation, and induction of apoptosis. In contrast, neither drug was effective against HMC-1.2 cells at the dose range tested. The present results suggest clinical potential for INNO-406 in KIT V560G-expressing malignancies.

Original languageEnglish (US)
Pages (from-to)1223-1225
Number of pages3
JournalCancer Science
Volume98
Issue number8
DOIs
Publication statusPublished - Aug 1 2007
Externally publishedYes

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ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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