Journal article
Complete remission of TEL-PDGFRB–induced myeloproliferative disease in mice by receptor tyrosine kinase inhibitor SU11657
Blood, Vol.104(2), pp.561-564
07/15/2004
DOI: 10.1182/blood-2003-11-3801
PMID: 15044254
Abstract
Abstract The TEL-PDGFRB fusion oncogene is associated with chronic myelomonocytic leukemia (CMML) and results in the expression of a constitutively active tyrosine kinase. SU11657 is a multitargeted selective inhibitor of class III/V receptor tyrosine kinases, including the platelet-derived growth factor (PDGF) and vascular endothelial growth factor (VEGF) receptors KIT and FLT3. SU11657 inhibited TEL/PDGFβR kinase activity at nanomolar concentrations and inhibited TELPDGFRB-mediated factor-independent growth in myeloblastic 32D cells. Daily oral administration of SU11657 at 40 mg/kg suppressed myeloproliferation and significantly prolonged survival in TELPDGFRB mice treated prior to disease development, as well as in those with large tumor burdens. Our findings suggest that SU11657 or similar agents may have therapeutic potential in humans with hematologic malignancies expressing PDGFR fusion oncogenes. (Blood. 2004;104:561-564)
Details
- Title: Subtitle
- Complete remission of TEL-PDGFRB–induced myeloproliferative disease in mice by receptor tyrosine kinase inhibitor SU11657
- Creators
- Jennifer A Cain - From the Division of Oncology, Departments of Medicine and Genetics, Siteman Cancer Center, Washington University School of Medicine, St Louis, MO; and Preclinical Research and Exploratory Development, SUGEN Inc, South San Francisco, CAJay L Grisolano - From the Division of Oncology, Departments of Medicine and Genetics, Siteman Cancer Center, Washington University School of Medicine, St Louis, MO; and Preclinical Research and Exploratory Development, SUGEN Inc, South San Francisco, CAA. Douglas Laird - From the Division of Oncology, Departments of Medicine and Genetics, Siteman Cancer Center, Washington University School of Medicine, St Louis, MO; and Preclinical Research and Exploratory Development, SUGEN Inc, South San Francisco, CAMichael H Tomasson - From the Division of Oncology, Departments of Medicine and Genetics, Siteman Cancer Center, Washington University School of Medicine, St Louis, MO; and Preclinical Research and Exploratory Development, SUGEN Inc, South San Francisco, CA
- Resource Type
- Journal article
- Publication Details
- Blood, Vol.104(2), pp.561-564
- DOI
- 10.1182/blood-2003-11-3801
- PMID
- 15044254
- NLM abbreviation
- Blood
- ISSN
- 0006-4971
- eISSN
- 1528-0020
- Language
- English
- Date published
- 07/15/2004
- Academic Unit
- Hematology, Oncology, and Blood & Marrow Transplantation; Internal Medicine
- Record Identifier
- 9984094530602771
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