Thursday, July 25, 2013
Publication and contact
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
All contents Copyright © 1993-2015 BioCentury Publications, Inc. ALL RIGHTS RESERVED. All use of this Web Site and its contents is governed by the BioCentury User Agreement
. The contents of this Web Site are protected under U.S. and foreign copyright and intellectual property laws, and no part of this Web Site or its contents may be photocopied, reproduced or retransmitted in any form without the written consent of BioCentury, which may be requested from Reprints/Permissions
. BioCentury®; The Bernstein Report on BioBusiness™; The BioCentury 100™; The Clear Route to ROI™; Because Real Intelligence is Hard to Find™; BCIQ™; and BioPharma's Knowledge Center™; are trademarks of BioCentury Publications, Inc., P.O. Box 1246, San Carlos, CA 94070. SciBX® and SciBX: Science-Business eXchange® are trademarks of Nature America, Inc. that are jointly used by BioCentury Publications, Inc. and Nature America, Inc.
Thanks for purchasing this article.
Please bookmark this url for future reference.
We have also sent you a confirming e-mail with a receipt and this same url for your
close [ X ]