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[Cancer Research 56, 100-104, January 1, 1996]
© 1996 American Association for Cancer Research
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Inhibition of the Abl Protein-Tyrosine Kinase in Vitro and in Vivo by a 2-Phenylaminopyrimidine Derivative

Elisabeth Buchdunger1, Jürg Zimmermann, Helmut Mett, Thomas Meyer, Marcel Müller, Brian J. Druker and Nicholas B. Lydon

Ciba Pharmaceuticals Division, Oncology Research Department, Ciba-Geigy Limited, CH-4002 Basel, Switzerland [E. B., J. Z., H. M., T. M., M. M., N. B. L.], and Division of Hematology and Medical Oncology, Oregon Health Sciences University, Portland, Oregon 97201 [B. J. D.]

Oncogenic activation of Abl proteins due to structural modifications can occur as a result of viral transduction or chromosomal translocation. The tyrosine protein kinase activity of oncogenic Abl proteins is known to be essential for their transforming activity. Therefore, we have attempted to identify selective inhibitors of the Abl tyrosine protein kinase. Herein we describe an inhibitor (CGP 57148) of the Abl and platelet-derived growth factor (PDGF) receptor protein-tyrosine kinases from the 2-phenylaminopyrimidine class, which is highly active in vitro and in vivo. Submicromolar concentrations of the compound inhibited both v-Abl and PDGF receptor autophosphorylation and PDGF-induced c-fos mRNA expression selectively in intact cells. In contrast, ligand-induced growth factor receptor autophosphorylation in response to epidermal growth factor (EGF), insulin-like growth factor-I, and insulin showed no or weak inhibition by high concentrations of CGP 57148. c-fos mRNA expression induced by EGF, fibroblast growth factor, or phorbol ester was also insensitive to inhibition by CGP 57148. In antiproliferative assays, the compound was more than 30–100-fold more potent in inhibiting growth of v-abl-transformed PB-3c cells and v-sis-transformed BALB/c 3T3 cells relative to inhibition of EGF-dependent BALB/MK cells, interleukin-3-dependent FDC-P1 cells, and the T24 bladder carcinoma line. Furthermore, anchorage-independent growth of v-abl- and v-sis-transformed BALB/c 3T3 cells was inhibited potently by CGP 57148. When tested in vivo, CGP 57148 showed antitumor activity at tolerated doses against tumorigenic v-abl- and v-sis-transformed BALB/c 3T3 cells. In contrast, CGP 57148 had no antitumor activity when tested using src-transformed BALB/c 3T3 cells. These findings suggest that CGP 57148 may have therapeutic potential for the treatment of diseases that involve abnormal cellular proliferation induced by Abl protein-tyrosine kinase deregulation or PDGF receptor activation.

1 To whom requests for reprints should be addressed, at Ciba Pharmaceuticals Division, Research Department, Ciba-Geigy Limited, CH-4002 Basel, Switzerland. Phone: 061/6962853 or 061/6964498; Fax: 061/6963835.

Received 7/31/95. Accepted 10/31/95.




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[Abstract] [Full Text] [PDF]

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 BloodHome page
M. Deininger, E. Buchdunger, and B. J. Druker
The development of imatinib as a therapeutic agent for chronic myeloid leukemia
Blood, April 1, 2005; 105(7): 2640 - 2653.
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A. Tefferi, G. W. Dewald, M. L. Litzow, J. Cortes, M. J. Mauro, M. Talpaz, and H. M. Kantarjian
Chronic Myeloid Leukemia: Current Application of Cytogenetics and Molecular Testing for Diagnosis and Treatment
Mayo Clin. Proc., March 1, 2005; 80(3): 390 - 402.
[Abstract] [PDF]

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 JCOHome page
K. Pietras and D. Hanahan
A Multitargeted, Metronomic, and Maximum-Tolerated Dose "Chemo-Switch" Regimen is Antiangiogenic, Producing Objective Responses and Survival Benefit in a Mouse Model of Cancer
J. Clin. Oncol., February 10, 2005; 23(5): 939 - 952.
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M. Lassila, K. Jandeleit-Dahm, K. K. Seah, C. M. Smith, A. C. Calkin, T. J. Allen, and M. E. Cooper
Imatinib Attenuates Diabetic Nephropathy in Apolipoprotein E-Knockout Mice
J. Am. Soc. Nephrol., February 1, 2005; 16(2): 363 - 373.
[Abstract] [Full Text] [PDF]

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 BloodHome page
F. Guo, C. Sigua, P. Bali, P. George, W. Fiskus, A. Scuto, S. Annavarapu, A. Mouttaki, G. Sondarva, S. Wei, et al.
Mechanistic role of heat shock protein 70 in Bcr-Abl-mediated resistance to apoptosis in human acute leukemia cells
Blood, February 1, 2005; 105(3): 1246 - 1255.
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S. Wang, M. C. Wilkes, E. B. Leof, and R. Hirschberg
Imatinib mesylate blocks a non-Smad TGF-{beta} pathway and reduces renal fibrogenesis in vivo
FASEB J, January 1, 2005; 19(1): 1 - 11.
[Abstract] [Full Text] [PDF]

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 Clin. Cancer Res.Home page
D. C. Lev, S. J. Kim, A. Onn, V. Stone, D.-H. Nam, S. Yazici, I. J. Fidler, and J. E. Price
Inhibition of Platelet-Derived Growth Factor Receptor Signaling Restricts the Growth of Human Breast Cancer in the Bone of Nude Mice
Clin. Cancer Res., January 1, 2005; 11(1): 306 - 314.
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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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M. Baccarani, G. Martinelli, G. Rosti, E. Trabacchi, N. Testoni, S. Bassi, M. Amabile, S. Soverini, F. Castagnetti, D. Cilloni, et al.
Imatinib and pegylated human recombinant interferon-{alpha}2b in early chronic-phase chronic myeloid leukemia
Blood, December 15, 2004; 104(13): 4245 - 4251.
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H. Choi, C. Charnsangavej, S. d. C. Faria, E. P. Tamm, R. S. Benjamin, M. M. Johnson, H. A. Macapinlac, and D. A. Podoloff
CT Evaluation of the Response of Gastrointestinal Stromal Tumors After Imatinib Mesylate Treatment: A Quantitative Analysis Correlated with FDG PET Findings
Am. J. Roentgenol., December 1, 2004; 183(6): 1619 - 1628.
[Abstract] [Full Text] [PDF]

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 BloodHome page
J. Thomas, L. Wang, R. E. Clark, and M. Pirmohamed
Active transport of imatinib into and out of cells: implications for drug resistance
Blood, December 1, 2004; 104(12): 3739 - 3745.
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 Mol. Cell. Biol.Home page
S. Fernandez de Mattos, A. Essafi, I. Soeiro, A. M. Pietersen, K. U. Birkenkamp, C. S. Edwards, A. Martino, B. H. Nelson, J. M. Francis, M. C. Jones, et al.
FoxO3a and BCR-ABL Regulate cyclin D2 Transcription through a STAT5/BCL6-Dependent Mechanism
Mol. Cell. Biol., November 15, 2004; 24(22): 10058 - 10071.
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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.
[Abstract] [Full Text] [PDF]

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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.
[Abstract] [Full Text] [PDF]

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S. B. Jones, H. Y. Lu, and Q. Lu
Abl Tyrosine Kinase Promotes Dendrogenesis by Inducing Actin Cytoskeletal Rearrangements in Cooperation with Rho Family Small GTPases in Hippocampal Neurons
J. Neurosci., September 29, 2004; 24(39): 8510 - 8521.
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D. J. DeAngelo, E. P. Hochberg, E. P. Alyea, J. Longtine, S. Lee, I. Galinsky, B. Parekkedon, J. Ritz, J. H. Antin, R. M. Stone, et al.
Extended Follow-up of Patients Treated with Imatinib Mesylate (Gleevec) for Chronic Myelogenous Leukemia Relapse after Allogeneic Transplantation: Durable Cytogenetic Remission and Conversion to Complete Donor Chimerism without Graft-versus-Host Disease
Clin. Cancer Res., August 1, 2004; 10(15): 5065 - 5071.
[Abstract] [Full Text] [PDF]

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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.
[Abstract] [Full Text] [PDF]

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J. Zhu, J.-W. Huang, P.-H. Tseng, Y.-T. Yang, J. Fowble, C.-W. Shiau, Y.-J. Shaw, S. K. Kulp, and C.-S. Chen
From the Cyclooxygenase-2 Inhibitor Celecoxib to a Novel Class of 3-Phosphoinositide-Dependent Protein Kinase-1 Inhibitors
Cancer Res., June 15, 2004; 64(12): 4309 - 4318.
[Abstract] [Full Text] [PDF]

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 BloodHome page
M. Mohty, E. Jourdan, N. B. Mami, N. Vey, G. Damaj, D. Blaise, D. Isnardon, D. Olive, and B. Gaugler
Imatinib and plasmacytoid dendritic cell function in patients with chronic myeloid leukemia
Blood, June 15, 2004; 103(12): 4666 - 4668.
[Abstract] [Full Text] [PDF]

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S. Parmar, E. Katsoulidis, A. Verma, Y. Li, A. Sassano, L. Lal, B. Majchrzak, F. Ravandi, M. S. Tallman, E. N. Fish, et al.
Role of the p38 Mitogen-activated Protein Kinase Pathway in the Generation of the Effects of Imatinib Mesylate (STI571) in BCR-ABL-expressing Cells
J. Biol. Chem., June 11, 2004; 279(24): 25345 - 25352.
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 The OncologistHome page
F. Guilhot
Indications for Imatinib Mesylate Therapy and Clinical Management
Oncologist, June 1, 2004; 9(3): 271 - 281.
[Abstract] [Full Text] [PDF]

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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.
[Abstract] [Full Text] [PDF]

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 JCBHome page
Y. H. Lin, Z.-Y. Park, D. Lin, A. A. Brahmbhatt, M.-C. Rio, J. R. Yates III, and R. L. Klemke
Regulation of cell migration and survival by focal adhesion targeting of Lasp-1
J. Cell Biol., May 10, 2004; 165(3): 421 - 432.
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 J. Clin. Endocrinol. Metab.Home page
J. M. Dziba and K. B. Ain
Imatinib Mesylate (Gleevec; STI571) Monotherapy Is Ineffective in Suppressing Human Anaplastic Thyroid Carcinoma Cell Growth in Vitro
J. Clin. Endocrinol. Metab., May 1, 2004; 89(5): 2127 - 2135.
[Abstract] [Full Text] [PDF]

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 Cancer Res.Home page
M. Furuhashi, T. Sjoblom, A. Abramsson, J. Ellingsen, P. Micke, H. Li, E. Bergsten-Folestad, U. Eriksson, R. Heuchel, C. Betsholtz, et al.
Platelet-Derived Growth Factor Production by B16 Melanoma Cells Leads to Increased Pericyte Abundance in Tumors and an Associated Increase in Tumor Growth Rate
Cancer Res., April 15, 2004; 64(8): 2725 - 2733.
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M. Cataldi, A. Gaudino, V. Lariccia, M. Russo, S. Amoroso, G. di Renzo, and L. Annunziato
Imatinib-Mesylate Blocks Recombinant T-Type Calcium Channels Expressed in Human Embryonic Kidney-293 Cells by a Protein Tyrosine Kinase-Independent Mechanism
J. Pharmacol. Exp. Ther., April 1, 2004; 309(1): 208 - 215.
[Abstract] [Full Text]

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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.
[Abstract] [Full Text] [PDF]

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B. Peng, M. Hayes, D. Resta, A. Racine-Poon, B. J. Druker, M. Talpaz, C. L. Sawyers, M. Rosamilia, J. Ford, P. Lloyd, et al.
Pharmacokinetics and Pharmacodynamics of Imatinib in a Phase I Trial With Chronic Myeloid Leukemia Patients
J. Clin. Oncol., March 1, 2004; 22(5): 935 - 942.
[Abstract] [Full Text] [PDF]

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 Clin. Cancer Res.Home page
D. Matei, D. D. Chang, and M.-H. Jeng
Imatinib Mesylate (Gleevec) Inhibits Ovarian Cancer Cell Growth through a Mechanism Dependent on Platelet-Derived Growth Factor Receptor {alpha} and Akt Inactivation
Clin. Cancer Res., January 15, 2004; 10(2): 681 - 690.
[Abstract] [Full Text] [PDF]

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 BloodHome page
K. Bartolovic, S. Balabanov, U. Hartmann, M. Komor, A. M. Boehmler, H.-J. Buhring, R. Mohle, D. Hoelzer, L. Kanz, W.-K. Hofmann, et al.
Inhibitory effect of imatinib on normal progenitor cells in vitro
Blood, January 15, 2004; 103(2): 523 - 529.
[Abstract] [Full Text] [PDF]

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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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E. J. Noronha, K. H. Sterling, and K. L. Calame
Increased Expression of Bcl-xL and c-Myc Is Associated with Transformation by Abelson Murine Leukemia Virus
J. Biol. Chem., December 19, 2003; 278(51): 50915 - 50922.
[Abstract] [Full Text] [PDF]

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 BloodHome page
P. T. Ferrao, M. J. Frost, S.-P. Siah, and L. K. Ashman
Overexpression of P-glycoprotein in K562 cells does not confer resistance to the growth inhibitory effects of imatinib (STI571) in vitro
Blood, December 15, 2003; 102(13): 4499 - 4503.
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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.
[Abstract] [Full Text] [PDF]

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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.
[Abstract] [Full Text]

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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.
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 Cancer Res.Home page
S. Matsuyama, M. Iwadate, M. Kondo, M. Saitoh, A. Hanyu, K. Shimizu, H. Aburatani, H. K. Mishima, T. Imamura, K. Miyazono, et al.
SB-431542 and Gleevec Inhibit Transforming Growth Factor-{beta}-Induced Proliferation of Human Osteosarcoma Cells
Cancer Res., November 15, 2003; 63(22): 7791 - 7798.
[Abstract] [Full Text] [PDF]

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 Mol Cancer ResHome page
K. M. Kirschner and K. Baltensperger
Erythropoietin Promotes Resistance Against the Abl Tyrosine Kinase Inhibitor Imatinib (STI571) in K562 Human Leukemia Cells
Mol. Cancer Res., November 1, 2003; 1(13): 970 - 980.
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 Clin. Cancer Res.Home page
H. Pfeifer, B. Wassmann, W.-K. Hofmann, M. Komor, U. Scheuring, P. Bruck, A. Binckebanck, E. Schleyer, N. Gokbuget, T. Wolff, et al.
Risk and Prognosis of Central Nervous System Leukemia in Patients with Philadelphia Chromosome-Positive Acute Leukemias Treated with Imatinib Mesylate
Clin. Cancer Res., October 15, 2003; 9(13): 4674 - 4681.
[Abstract] [Full Text] [PDF]


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