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Blood, Vol. 96 No. 3 (August 1), 2000: pp. 925-932

Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor

Michael C. Heinrich, Diana J. Griffith, Brian J. Druker, Cecily L. Wait, Kristen A. Ott, and Amy J. Zigler

From the Division of Hematology and Medical Oncology, Department of Medicine, Oregon Health Sciences University, and Portland Veterans Affairs Medical Center, Portland, OR.

STI 571 (formerly known as CGP 57148B) is a known inhibitor of the c-abl, bcr-abl, and platelet-derived growth-factor receptor (PDGFR) tyrosine kinases. This compound is being evaluated in clinical trials for the treatment of chronic myelogenous leukemia. We sought to extend the activity profile of STI 571 by testing its ability to inhibit the tyrosine kinase activity of c-kit, a receptor structurally similar to PDGFR. We treated a c-kit expressing a human myeloid leukemia cell line, M-07e, with STI 571 before stimulation with Steel factor (SLF). STI 571 inhibited c-kit autophosphorylation, activation of mitogen-activated protein (MAP) kinase, and activation of Akt without altering total protein levels of c-kit, MAP kinase, or Akt. The concentration that produced 50% inhibition for these effects was approximately 100 nmol/L. STI 571 also significantly decreased SLF-dependent growth of M-07e cells in a dose-dependent manner and blocked the antiapoptotic activity of SLF. In contrast, the compound had no effect on MAP kinase activation or cellular proliferation in response to granulocyte-macrophage colony-stimulating factor. We also tested the activity of STI 571 in a human mast cell leukemia cell line (HMC-1), which has an activated mutant form of c-kit. STI 571 had a more potent inhibitory effect on the kinase activity of this mutant receptor than it did on ligand-dependent activation of the wild-type receptor. These findings show that STI 571 selectively inhibits c-kit tyrosine kinase activity and downstream activation of target proteins involved in cellular proliferation and survival. This compound may be useful in treating cancers associated with increased c-kit kinase activity.


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S. Uccini, O. Mannarino, H. P. McDowell, U. Pauser, R. Vitali, P. G. Natali, P. Altavista, T. Andreano, S. Coco, R. Boldrini, et al.
Clinical and Molecular Evidence for c-kit Receptor as a Therapeutic Target in Neuroblastic Tumors
Clin. Cancer Res., January 1, 2005; 11(1): 380 - 389.
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ASH Education BookHome page
R. L. Ilaria Jr.
Pathobiology of Lymphoid and Myeloid Blast Crisis and Management Issues
Hematology, January 1, 2005; 2005(1): 188 - 194.
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Mayo Clin Proc.Home page
A. Tefferi
Blood Eosinophilia: A New Paradigm in Disease Classification, Diagnosis, and Treatment
Mayo Clin. Proc., January 1, 2005; 80(1): 75 - 83.
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BloodHome page
K. W. H. Yee, M. Schittenhelm, A.-M. O'Farrell, A. R. Town, L. McGreevey, T. Bainbridge, J. M. Cherrington, and M. C. Heinrich
Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells
Blood, December 15, 2004; 104(13): 4202 - 4209.
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J. Biol. Chem.Home page
P. Kempna, E. Reiter, M. Arock, A. Azzi, and J.-M. Zingg
Inhibition of HMC-1 Mast Cell Proliferation by Vitamin E: INVOLVEMENT OF THE PROTEIN KINASE B PATHWAY
J. Biol. Chem., December 3, 2004; 279(49): 50700 - 50709.
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BloodHome page
A. S. Corbin, I. J. Griswold, P. La Rosee, K. W. H. Yee, M. C. Heinrich, C. L. Reimer, B. J. Druker, and M. W. N. Deininger
Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970
Blood, December 1, 2004; 104(12): 3754 - 3757.
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J EndocrinolHome page
J A Fagin
How thyroid tumors start and why it matters: kinase mutants as targets for solid cancer pharmacotherapy
J. Endocrinol., November 1, 2004; 183(2): 249 - 256.
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NEJMHome page
G. D. Demetri, R. L. Titton, D. P. Ryan, and C. D.M. Fletcher
Case 32-2004 - A 68-Year-Old Man with a Large Retroperitoneal Mass
N. Engl. J. Med., October 21, 2004; 351(17): 1779 - 1787.
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J. Biol. Chem.Home page
A. Ertmer, S. Gilch, S.-W. Yun, E. Flechsig, B. Klebl, M. Stein-Gerlach, M. A. Klein, and H. M. Schatzl
The Tyrosine Kinase Inhibitor STI571 Induces Cellular Clearance of PrPSc in Prion-infected Cells
J. Biol. Chem., October 1, 2004; 279(40): 41918 - 41927.
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BloodHome page
A. Pardanani and A. Tefferi
Imatinib targets other than bcr/abl and their clinical relevance in myeloid disorders
Blood, October 1, 2004; 104(7): 1931 - 1939.
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JCOHome page
C. L. Corless, J. A. Fletcher, and M. C. Heinrich
Biology of Gastrointestinal Stromal Tumors
J. Clin. Oncol., September 15, 2004; 22(18): 3813 - 3825.
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Clin. Cancer Res.Home page
J. V. Heymach, J. Desai, J. Manola, D. W. Davis, D. J. McConkey, D. Harmon, D. P. Ryan, G. Goss, T. Quigley, A. D. Van den Abbeele, et al.
Phase II Study of the Antiangiogenic Agent SU5416 in Patients with Advanced Soft Tissue Sarcomas
Clin. Cancer Res., September 1, 2004; 10(17): 5732 - 5740.
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BloodHome page
A. B. Dietz, L. Souan, G. J. Knutson, P. A. Bulur, M. R. Litzow, and S. Vuk-Pavlovic
Imatinib mesylate inhibits T-cell proliferation in vitro and delayed-type hypersensitivity in vivo
Blood, August 15, 2004; 104(4): 1094 - 1099.
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JCOHome page
A. R. Tan, X. Yang, S. M. Hewitt, A. Berman, E. R. Lepper, A. Sparreboom, A. L. Parr, W. D. Figg, C. Chow, S. M. Steinberg, et al.
Evaluation of Biologic End Points and Pharmacokinetics in Patients With Metastatic Breast Cancer After Treatment With Erlotinib, an Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor
J. Clin. Oncol., August 1, 2004; 22(15): 3080 - 3090.
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J. Biol. Chem.Home page
G. Lefevre, A.-L. Glotin, A. Calipel, F. Mouriaux, T. Tran, Z. Kherrouche, C.-A. Maurage, C. Auclair, and F. Mascarelli
Roles of Stem Cell Factor/c-Kit and Effects of Glivec(R)/STI571 in Human Uveal Melanoma Cell Tumorigenesis
J. Biol. Chem., July 23, 2004; 279(30): 31769 - 31779.
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BloodHome page
L. Legros, C. Bourcier, A. Jacquel, F.-X. Mahon, J.-P. Cassuto, P. Auberger, and G. Pages
Imatinib mesylate (STI571) decreases the vascular endothelial growth factor plasma concentration in patients with chronic myeloid leukemia
Blood, July 15, 2004; 104(2): 495 - 501.
[Abstract] [Full Text] [PDF]


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Annals of Clinical & Laboratory ScienceHome page
P. L. Zhang, M. Lun, N. Siegelmann-Danieli, T. M. Blasick, and R. E. Brown
Pamidronate Resistance and Associated Low Ras Levels in Breast Cancer Cells: A Role for Combinatorial Therapy
Ann. Clin. Lab. Sci., July 1, 2004; 34(3): 263 - 270.
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IOVSHome page
C. All-Ericsson, L. Girnita, A. Muller-Brunotte, B. Brodin, S. Seregard, A. Ostman, and O. Larsson
c-Kit-Dependent Growth of Uveal Melanoma Cells: A Potential Therapeutic Target?
Invest. Ophthalmol. Vis. Sci., July 1, 2004; 45(7): 2075 - 2082.
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Cancer Res.Home page
R. R. Langley, D. Fan, R. Z. Tsan, R. Rebhun, J. He, S.-J. Kim, and I. J. Fidler
Activation of the Platelet-Derived Growth Factor-Receptor Enhances Survival of Murine Bone Endothelial Cells
Cancer Res., June 1, 2004; 64(11): 3727 - 3730.
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Mol. Pharmacol.Home page
C. Ozvegy-Laczka, T. Heged""s, G. Varady, O. Ujhelly, J. D. Schuetz, A. Varadi, G. Keri, L. Orfi, K. Nemet, and B. Sarkadi
High-Affinity Interaction of Tyrosine Kinase Inhibitors with the ABCG2 Multidrug Transporter
Mol. Pharmacol., June 1, 2004; 65(6): 1485 - 1495.
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Clin. Cancer Res.Home page
N. C. Wolff, D. E. Randle, M. J. Egorin, J. D. Minna, and R. L. Ilaria Jr.
Imatinib Mesylate Efficiently Achieves Therapeutic Intratumor Concentrations in Vivo but Has Limited Activity in a Xenograft Model of Small Cell Lung Cancer
Clin. Cancer Res., May 15, 2004; 10(10): 3528 - 3534.
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Ann. Surg. Oncol.Home page
B. L. Eisenberg and I. Judson
Surgery and Imatinib in the Management of GIST: Emerging Approaches to Adjuvant and Neoadjuvant Therapy
Ann. Surg. Oncol., May 1, 2004; 11(5): 465 - 475.
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Cancer Res.Home page
S. S. Castillo, J. Brognard, P. A. Petukhov, C. Zhang, J. Tsurutani, C. A. Granville, M. Li, M. Jung, K. A. West, J. G. Gills, et al.
Preferential Inhibition of Akt and Killing of Akt-Dependent Cancer Cells by Rationally Designed Phosphatidylinositol Ether Lipid Analogues
Cancer Res., April 15, 2004; 64(8): 2782 - 2792.
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INT J SURG PATHOLHome page
J. L. Hornick and C. D. M. Fletcher
The Significance of KIT (CD117) in Gastrointestinal Stromal Tumors
International Journal of Surgical Pathology, April 1, 2004; 12(2): 93 - 97.
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Ann OncolHome page
M. R. Raspollini, G. Amunni, A. Villanucci, G. Baroni, A. Taddei, and G. L. Taddei
c-KIT expression and correlation with chemotherapy resistance in ovarian carcinoma: an immunocytochemical study
Ann. Onc., April 1, 2004; 15(4): 594 - 597.
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Clin. Cancer Res.Home page
K. Neville, R. A. Parise, P. Thompson, A. Aleksic, M. J. Egorin, F. M. Balis, L. McGuffey, C. McCully, S. L. Berg, and S. M. Blaney
Plasma and Cerebrospinal Fluid Pharmacokinetics of Imatinib after Administration to Nonhuman Primates
Clin. Cancer Res., April 1, 2004; 10(7): 2525 - 2529.
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ScienceHome page
M. E. M. Noble, J. A. Endicott, and L. N. Johnson
Protein Kinase Inhibitors: Insights into Drug Design from Structure
Science, March 19, 2004; 303(5665): 1800 - 1805.
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BloodHome page
G. Rosti, G. Martinelli, S. Bassi, M. Amabile, E. Trabacchi, B. Giannini, D. Cilloni, B. Izzo, A. De Vivo, N. Testoni, et al.
Molecular response to imatinib in late chronic-phase chronic myeloid leukemia
Blood, March 15, 2004; 103(6): 2284 - 2290.
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JNMHome page
G. Antoch, J. Kanja, S. Bauer, H. Kuehl, K. Renzing-Koehler, J. Schuette, A. Bockisch, J. F. Debatin, and L. S. Freudenberg
Comparison of PET, CT, and Dual-Modality PET/CT Imaging for Monitoring of Imatinib (STI571) Therapy in Patients with Gastrointestinal Stromal Tumors
J. Nucl. Med., March 1, 2004; 45(3): 357 - 365.
[Abstract] [Full Text]


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BloodHome page
S. Appel, A. M. Boehmler, F. Grunebach, M. R. Muller, A. Rupf, M. M. Weck, U. Hartmann, V. L. Reichardt, L. Kanz, T. H. Brummendorf, et al.
Imatinib mesylate affects the development and function of dendritic cells generated from CD34+ peripheral blood progenitor cells
Blood, January 15, 2004; 103(2): 538 - 544.
[Abstract] [Full Text] [PDF]


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JNMHome page
I. Gayed, T. Vu, R. Iyer, M. Johnson, H. Macapinlac, N. Swanston, and D. Podoloff
The Role of 18F-FDG PET in Staging and Early Prediction of Response to Therapy of Recurrent Gastrointestinal Stromal Tumors
J. Nucl. Med., January 1, 2004; 45(1): 17 - 21.
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K. Kemmer, C. L. Corless, J. A. Fletcher, L. McGreevey, A. Haley, D. Griffith, O. W. Cummings, C. Wait, A. Town, and M. C. Heinrich
KIT Mutations Are Common in Testicular Seminomas
Am. J. Pathol., January 1, 2004; 164(1): 305 - 313.
[Abstract] [Full Text] [PDF]


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BloodHome page
G. Z. Rassidakis, G. V. Georgakis, A. Younes, and L. J. Medeiros
c-kit is not expressed in Hodgkin disease and anaplastic lymphoma kinase (ALK)-positive anaplastic large cell lymphoma
Blood, December 15, 2003; 102(13): 4619 - 4620.
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JCOHome page
M. C. Heinrich, C. L. Corless, G. D. Demetri, C. D. Blanke, M. von Mehren, H. Joensuu, L. S. McGreevey, C.-J. Chen, A. D. Van den Abbeele, B. J. Druker, et al.
Kinase Mutations and Imatinib Response in Patients With Metastatic Gastrointestinal Stromal Tumor
J. Clin. Oncol., December 1, 2003; 21(23): 4342 - 4349.
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K. Takeuchi, K. Koike, T. Kamijo, S. Ishida, Y. Nakazawa, Y. Kurokawa, K. Sakashita, T. Kinoshita, S. Matsuzawa, M. Shiohara, et al.
STI571 inhibits growth and adhesion of human mast cells in culture
J. Leukoc. Biol., December 1, 2003; 74(6): 1026 - 1034.
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Clin. Cancer Res.Home page
B. E. Johnson, T. Fischer, B. Fischer, D. Dunlop, D. Rischin, S. Silberman, M. O. Kowalski, D. Sayles, S. Dimitrijevic, C. Fletcher, et al.
Phase II Study of Imatinib in Patients with Small Cell Lung Cancer
Clin. Cancer Res., December 1, 2003; 9(16): 5880 - 5887.
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BloodHome page
T. Grunberger, P. Demin, O. Rounova, N. Sharfe, L. Cimpean, H. Dadi, A. Freywald, Z. Estrov, and C. M. Roifman
Inhibition of acute lymphoblastic and myeloid leukemias by a novel kinase inhibitor
Blood, December 1, 2003; 102(12): 4153 - 4158.
[Abstract] [Full Text] [PDF]


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BloodHome page
M. F. McMullin, M. Humphreys, J. Byrne, N. H. Russell, R. J. Cuthbert, M. E. O'Dwyer, H.-K. Al-Ali, T. Bumm, C. Muller, P. Shepherd, et al.
Chromosomal abnormalities in Ph- cells of patients on imatinib
Blood, October 1, 2003; 102(7): 2700 - 2701.
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Molecular Cancer TherapeuticsHome page
A. Frolov, S. Chahwan, M. Ochs, J. P. Arnoletti, Z.-Z. Pan, O. Favorova, J. Fletcher, M. von Mehren, B. Eisenberg, and A. K. Godwin
Response Markers and the Molecular Mechanisms of Action of Gleevec in Gastrointestinal Stromal Tumors
Mol. Cancer Ther., August 1, 2003; 2(8): 699 - 709.
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JCOHome page
K. Scotlandi, M. C. Manara, R. Strammiello, L. Landuzzi, S. Benini, S. Perdichizzi, M. Serra, A. Astolfi, G. Nicoletti, P.-L. Lollini, et al.
c-kit Receptor Expression in Ewing's Sarcoma: Lack of Prognostic Value but Therapeutic Targeting Opportunities in Appropriate Conditions
J. Clin. Oncol., May 15, 2003; 21(10): 1952 - 1960.
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