Thursday, July 25, 2013
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Stem cell factor receptor tyrosine kinase (c-Kit;
KIT inhibitors could help treat Gleevec
imatinib-resistant gastrointestinal stromal tumors (GISTs). Chemical
synthesis, SAR and in vitro testing identified
quinazoline-pyrazolourea analogs that inhibited wild-type KIT and two
imatinib-resistant KIT mutants with low nanomolar IC50 values. In
human GIST cell lines expressing constitutively active KIT or the imatinib-resistant
T670I KIT mutant, 3 of the lead compounds caused 50% growth inhibition at low
nanomolar concentrations. Future studies could include testing the lead
compounds in animal models bearing imatinib-resistant GIST xenografts.
AG markets Gleevec, a BCR-ABL
tyrosine kinase inhibitor, to treat GISTs, acute
lymphoblastic leukemia (ALL), chronic myelogenous leukemia (CML) and other
hematological malignancies. The drug also is under review for hypertension
and in Phase II testing to treat melanoma and scleroderma.
AB Science S.A.'s KIT
is under review for imatinib-resistant GISTs and in Phase III testing to
treat other cancers.
Published online July 25, 2013
Patent and licensing status
Richters, A. et al. J.
published online June 17, 2013;
Contact: Daniel Rauh, Technical University of Dortmund,
Contact: Sebastian Bauer, University of Duisburg-Essen
Medical School, Essen, Germany
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