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Prepublished online as a Blood First Edition Paper on January 16, 2003; DOI 10.1182/blood-2002-07-2307. This Article Full Text Full Text (PDF) All Versions of this Article: 2002-07-2307v1 101/9/3597    most recent Alert me when this article is cited Alert me if a correction is posted Citation Map Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Rights and Permissions Citing Articles Citing Articles via HighWire Citing Articles via CrossRef Citing Articles via Google Scholar Google Scholar Articles by O'Farrell, A.-M. Articles by Cherrington, J. M. Search for Related Content PubMed PubMed Citation Articles by O'Farrell, A.-M. Articles by Cherrington, J. M. Related Collections Neoplasia Oncogenes and Tumor Suppressors Signal Transduction Social Bookmarking                   What's this?  Previous Article  |  Table of Contents  |  Next Article  Blood, 1 May 2003, Vol. 101, No. 9, pp. 3597-3605 NEOPLASIA SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo Anne-Marie O'Farrell, Tinya J. Abrams, Helene A. Yuen, Theresa J. Ngai, Sharianne G. Louie, Kevin W. H. Yee, Lily M. Wong, Weiru Hong, Leslie B. Lee, Ajia Town, Beverly D. Smolich, William C. Manning, Lesley J. Murray, Michael C. Heinrich, and Julie M. Cherrington From Preclinical Research and Exploratory Development, SUGEN, South San Francisco, CA; and the Department of Medicine and Oregon Health and Science University (OHSU) Cancer Institute, Division of Hematology and Medical Oncology, OHSU and Portland Veterans Affairs Medical Center, OR. FLT3 (fms-related tyrosine kinase/Flk2/Stk-2) is a receptor tyrosine kinase (RTK) primarily expressed on hematopoietic cells. In blasts from acute myelogenous leukemia (AML) patients, 2 classes of FLT3 activating mutations have been identified: internal tandem duplication (ITD) mutations in the juxtamembrane domain (25%-30% of patients) and point mutations in the kinase domain activation loop (7%-8% of patients). FLT3-ITD mutations are the most common molecular defect identified in AML and have been shown to be an independent prognostic factor for decreased survival. FLT3-ITD is therefore an attractive molecular target for therapy. SU11248 is a recently described selective inhibitor with selectivity for split kinase domain RTKs, including platelet-derived growth factor receptors, vascular endothelial growth factor receptors, and KIT. We show that SU11248 also has potent activity against wild-type FLT3 (FLT3-WT), FLT3-ITD, and FLT3 activation loop (FLT3-Asp835) mutants in phosphorylation assays. SU11248 inhibits FLT3-driven phosphorylation and induces apoptosis in vitro. In addition, SU11248 inhibits FLT3-induced VEGF production. The in vivo efficacy of SU11248 was investigated in 2 FLT3-ITD models: a subcutaneous tumor xenograft model and a bone marrow engraftment model. We show that SU11248 (20 mg/kg/d) dramatically regresses FLT3-ITD tumors in the subcutaneous tumor xenograft model and prolongs survival in the bone marrow engraftment model. Pharmacokinetic and pharmacodynamic analysis in subcutaneous tumors showed that a single administration of an efficacious drug dose potently inhibits FLT3-ITD phosphorylation for up to 16 hours following a single dose. These results suggest that further exploration of SU11248 activity in AML patients is warranted. © 2003 by The American Society of Hematology.   CiteULike    Connotea    Del.icio.us    Digg    Reddit    Technorati    What's this? This article has been cited by other articles: R. Bao, C.-J. Lai, H. Qu, D. Wang, L. Yin, B. Zifcak, R. Atoyan, J. Wang, M. Samson, J. Forrester, et al. CUDC-305, a Novel Synthetic HSP90 Inhibitor with Unique Pharmacologic Properties for Cancer Therapy Clin. Cancer Res., June 15, 2009; 15(12): 4046 - 4057. [Abstract] [Full Text] [PDF] W. Castillo-Avila, J. M. Piulats, X. Garcia del Muro, A. Vidal, E. Condom, O. Casanovas, J. Mora, J. R. Germa, G. Capella, A. Villanueva, et al. Sunitinib Inhibits Tumor Growth and Synergizes with Cisplatin in Orthotopic Models of Cisplatin-Sensitive and Cisplatin-Resistant Human Testicular Germ Cell Tumors Clin. Cancer Res., May 15, 2009; 15(10): 3384 - 3395. [Abstract] [Full Text] [PDF] K. Burkitt, S. Y. Chun, D. T. 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