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[Cancer Research 60, 4152-4160, August 1, 2000]
© 2000 American Association for Cancer Research


Experimental Therapeutics

SU6668 Is a Potent Antiangiogenic and Antitumor Agent That Induces Regression of Established Tumors1

A. Douglas Laird, Peter Vajkoczy, Laura K. Shawver, Andreas Thurnher, Congxin Liang, Moosa Mohammadi, Joseph Schlessinger, Axel Ullrich, Stevan R. Hubbard, Robert A. Blake, T. Annie T. Fong, Laurie M. Strawn, Li Sun, Cho Tang, Rachael Hawtin, Flora Tang, Narmada Shenoy, K. Peter Hirth, Gerald McMahon and Julie M. Cherrington2

SUGEN, Inc., San Francisco, California 94080 [A. D. L., L. K. S., C. L., R. A. B., T. A. T. F., L. M. S., L. S., C. T., R. H., F. T., N. S., K. P. H., G. M., J. M. C.]; Department of Neurosurgery, Klinikum Mannheim, University of Heidelberg, D-68167 Mannheim, Germany [P. V., A. T.]; Department of Pharmacology, New York University Medical Center, New York, New York 10016 [M. M., J. S.]; Department of Molecular Biology, Max-Planck-Institut für Biochemie, D-82152 Martinsried, Germany [A. U.]; and Skirball Institute of Biomolecular Medicine and Department of Pharmacology, New York University Medical Center, New York, New York 10016 [S. R. H.]

Vascular endothelial growth factor, fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) and their cognate receptor tyrosine kinases are strongly implicated in angiogenesis associated with solid tumors. Using rational drug design coupled with traditional screening technologies, we have discovered SU6668, a novel inhibitor of these receptors. Biochemical kinetic studies using isolated Flk-1, FGF receptor 1, and PDGF receptor ß kinases revealed that SU6668 has competitive inhibitory properties with respect to ATP. Cocrystallographic studies of SU6668 in the catalytic domain of FGF receptor 1 substantiated the adenine mimetic properties of its oxindole core. Molecular modeling of SU6668 in the ATP binding pockets of the Flk-1/KDR and PDGF receptor kinases provided insight to explain the relative potency and selectivity of SU6668 for these receptors. In cellular systems, SU6668 inhibited receptor tyrosine phosphorylation and mitogenesis after stimulation of cells by appropriate ligands. Oral or i.p. administration of SU6668 in athymic mice resulted in significant growth inhibition of a diverse panel of human tumor xenografts of glioma, melanoma, lung, colon, ovarian, and epidermoid origin. Furthermore, intravital multifluorescence videomicroscopy of C6 glioma xenografts in the dorsal skinfold chamber model revealed that SU6668 treatment suppressed tumor angiogenesis. Finally, SU6668 treatment induced striking regression of large established human tumor xenografts. Investigations of SU6668 activity in cancer patients are ongoing in Phase I clinical trials.




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Src Family Kinase Activity Is Required for Signal Tranducer and Activator of Transcription 3 and Focal Adhesion Kinase Phosphorylation and Vascular Endothelial Growth Factor Signaling in Vivo and for Anchorage-dependent and -independent Growth of Human Tumor Cells
Mol. Cancer Ther., May 1, 2003; 2(5): 461 - 469.
[Abstract] [Full Text] [PDF]


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Clin. Cancer Res.Home page
C. L. Arteaga
Molecular Therapeutics: Is One Promiscuous Drug against Multiple Targets Better than Combinations of Molecule-specific Drugs?
Clin. Cancer Res., April 1, 2003; 9(4): 1231 - 1232.
[Full Text] [PDF]


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FASEB J.Home page
Y. ZHU, K. JIN, X. O. MAO, and D. A. GREENBERG
Vascular endothelial growth factor promotes proliferation of cortical neuron precursors by regulating E2F expression
FASEB J, February 1, 2003; 17(2): 186 - 193.
[Abstract] [Full Text] [PDF]


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The OncologistHome page
F. G. El Kamar, M. L. Grossbard, and P. S. Kozuch
Metastatic Pancreatic Cancer: Emerging Strategies in Chemotherapy and Palliative Care
Oncologist, February 1, 2003; 8(1): 18 - 34.
[Abstract] [Full Text] [PDF]


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Clin. Cancer Res.Home page
D. B. Mendel, A. D. Laird, X. Xin, S. G. Louie, J. G. Christensen, G. Li, R. E. Schreck, T. J. Abrams, T. J. Ngai, L. B. Lee, et al.
In Vivo Antitumor Activity of SU11248, a Novel Tyrosine Kinase Inhibitor Targeting Vascular Endothelial Growth Factor and Platelet-derived Growth Factor Receptors: Determination of a Pharmacokinetic/Pharmacodynamic Relationship
Clin. Cancer Res., January 1, 2003; 9(1): 327 - 337.
[Abstract] [Full Text] [PDF]


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J. Pharmacol. Exp. Ther.Home page
M. M. Belcheva, P. D. Haas, Y. Tan, V. M. Heaton, and C. J. Coscia
The Fibroblast Growth Factor Receptor Is at the Site of Convergence between {micro}-Opioid Receptor and Growth Factor Signaling Pathways in Rat C6 Glioma Cells
J. Pharmacol. Exp. Ther., December 1, 2002; 303(3): 909 - 918.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
X. Huang, M. K. Wong, H. Yi, S. Watkins, A. D. Laird, S. F. Wolf, and E. Gorelik
Combined Therapy of Local and Metastatic 4T1 Breast Tumor in Mice Using SU6668, an Inhibitor of Angiogenic Receptor Tyrosine Kinases, and the Immunostimulator B7.2-IgG Fusion Protein
Cancer Res., October 15, 2002; 62(20): 5727 - 5735.
[Abstract] [Full Text] [PDF]


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JNCI J Natl Cancer InstHome page
G. C. Jayson, J. Zweit, A. Jackson, C. Mulatero, P. Julyan, M. Ranson, L. Broughton, J. Wagstaff, L. Hakannson, G. Groenewegen, et al.
Molecular Imaging and Biological Evaluation of HuMV833 Anti-VEGF Antibody: Implications for Trial Design of Antiangiogenic Antibodies
J Natl Cancer Inst, October 2, 2002; 94(19): 1484 - 1493.
[Abstract] [Full Text] [PDF]


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BloodHome page
K. W. H. Yee, A. M. O'Farrell, B. D. Smolich, J. M. Cherrington, G. McMahon, C. L. Wait, L. S. McGreevey, D. J. Griffith, and M. C. Heinrich
SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase
Blood, September 26, 2002; 100(8): 2941 - 2949.
[Abstract] [Full Text] [PDF]


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JCOHome page
F. A. Scappaticci
Mechanisms and Future Directions for Angiogenesis-Based Cancer Therapies
J. Clin. Oncol., September 15, 2002; 20(18): 3906 - 3927.
[Abstract] [Full Text] [PDF]


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The OncologistHome page
C. J. Conti
Vascular Endothelial Growth Factor: Regulation in the Mouse Skin Carcinogenesis Model and Use in Antiangiogenesis Cancer Therapy
Oncologist, August 1, 2002; 7(90003): 4 - 11.
[Abstract] [Full Text] [PDF]


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BloodHome page
A. T. Liao, M. B. Chien, N. Shenoy, D. B. Mendel, G. McMahon, J. M. Cherrington, and C. A. London
Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors
Blood, June 28, 2002; 100(2): 585 - 593.
[Abstract] [Full Text] [PDF]


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J. Histochem. Cytochem.Home page
A. N. Witmer, J. Dai, H. A. Weich, G. F.J.M. Vrensen, and R. O. Schlingemann
Expression of Vascular Endothelial Growth Factor Receptors 1, 2, and 3 in Quiescent Endothelia
J. Histochem. Cytochem., June 1, 2002; 50(6): 767 - 778.
[Abstract] [Full Text] [PDF]


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Am. J. Pathol.Home page
H. Zhang and A. C. Issekutz
Down-Modulation of Monocyte Transendothelial Migration and Endothelial Adhesion Molecule Expression by Fibroblast Growth Factor : Reversal by the Anti-Angiogenic Agent SU6668
Am. J. Pathol., June 1, 2002; 160(6): 2219 - 2230.
[Abstract] [Full Text] [PDF]


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Proc. Natl. Acad. Sci. USAHome page
T. M. J. Niederman, Z. Ghogawala, B. S. Carter, H. S. Tompkins, M. M. Russell, and R. C. Mulligan
Antitumor activity of cytotoxic T lymphocytes engineered to target vascular endothelial growth factor receptors
PNAS, May 14, 2002; 99(10): 7009 - 7014.
[Abstract] [Full Text] [PDF]


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FASEB J.Home page
A. D. LAIRD, J. G. CHRISTENSEN, G. LI, J. CARVER, K. SMITH, X. XIN, K. G. MOSS, S. G. LOUIE, D. B. MENDEL, and J. M. CHERRINGTON
SU6668 inhibits Flk-1/KDR and PDGFR{beta} in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice
FASEB J, May 1, 2002; 16(7): 681 - 690.
[Abstract] [Full Text] [PDF]


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Clin. Cancer Res.Home page
R. Beliveau, D. Gingras, E. A. Kruger, S. Lamy, P. Sirois, B. Simard, M. G. Sirois, L. Tranqui, F. Baffert, E. Beaulieu, et al.
The Antiangiogenic Agent Neovastat (Ae-941) Inhibits Vascular Endothelial Growth Factor-mediated Biological Effects
Clin. Cancer Res., April 1, 2002; 8(4): 1242 - 1250.
[Abstract] [Full Text] [PDF]


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JCOHome page
M. C. Heinrich, C. D. Blanke, B. J. Druker, and C. L. Corless
Inhibition of KIT Tyrosine Kinase Activity: A Novel Molecular Approach to the Treatment of KIT-Positive Malignancies
J. Clin. Oncol., March 15, 2002; 20(6): 1692 - 1703.
[Abstract] [Full Text] [PDF]


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Eur Respir JHome page
C.S. Brock and S.M. Lee
Anti-angiogenic strategies and vascular targeting in the treatment of lung cancer
Eur. Respir. J., March 1, 2002; 19(3): 557 - 570.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
R. J. Griffin, B. W. Williams, R. Wild, J. M. Cherrington, H. Park, and C. W. Song
Simultaneous Inhibition of the Receptor Kinase Activity of Vascular Endothelial, Fibroblast, and Platelet-derived Growth Factors Suppresses Tumor Growth and Enhances Tumor Radiation Response
Cancer Res., March 1, 2002; 62(6): 1702 - 1706.
[Abstract] [Full Text] [PDF]


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Molecular Cancer TherapeuticsHome page
T. Itokawa, H. Nokihara, Y. Nishioka, S. Sone, Y. Iwamoto, Y. Yamada, J. Cherrington, G. McMahon, M. Shibuya, M. Kuwano, et al.
Antiangiogenic Effect by SU5416 Is Partly Attributable to Inhibition of Flt-1 Receptor Signaling
Mol. Cancer Ther., March 1, 2002; 1(5): 295 - 302.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
F. Carlomagno, D. Vitagliano, T. Guida, M. Napolitano, G. Vecchio, A. Fusco, A. Gazit, A. Levitzki, and M. Santoro
The Kinase Inhibitor PP1 Blocks Tumorigenesis Induced by RET Oncogenes
Cancer Res., February 1, 2002; 62(4): 1077 - 1082.
[Abstract] [Full Text] [PDF]


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JNCI J Natl Cancer InstHome page
M. Ozen, D. Giri, F. Ropiquet, A. Mansukhani, and M. Ittmann
Role of Fibroblast Growth Factor Receptor Signaling in Prostate Cancer Cell Survival
J Natl Cancer Inst, December 5, 2001; 93(23): 1783 - 1790.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
P. Guo, L. Xu, S. Pan, R. A. Brekken, S.-T. Yang, G. B. Whitaker, M. Nagane, P. E. Thorpe, J. S. Rosenbaum, H.-J. Su Huang, et al.
Vascular Endothelial Growth Factor Isoforms Display Distinct Activities in Promoting Tumor Angiogenesis at Different Anatomic Sites
Cancer Res., December 1, 2001; 61(23): 8569 - 8577.
[Abstract] [Full Text] [PDF]


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JCOHome page
R. S. Kerbel
Clinical Trials of Antiangiogenic Drugs: Opportunities, Problems, and Assessment of Initial Results
J. Clin. Oncol., September 15, 2001; 19(90001): 45s - 51.
[Full Text] [PDF]


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Cancer Res.Home page
G. W. Krystal, S. Honsawek, D. Kiewlich, C. Liang, S. Vasile, L. Sun, G. McMahon, and K. E. Lipson
Indolinone Tyrosine Kinase Inhibitors Block Kit Activation and Growth of Small Cell Lung Cancer Cells
Cancer Res., May 1, 2001; 61(9): 3660 - 3668.
[Abstract] [Full Text]


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Circ. Res.Home page
Y. Yamasaki, K. Miyoshi, N. Oda, M. Watanabe, H. Miyake, J. Chan, X. Wang, L. Sun, C. Tang, G. McMahon, et al.
Weekly Dosing With the Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitor SU9518 Significantly Inhibits Arterial Stenosis
Circ. Res., March 30, 2001; 88(6): 630 - 636.
[Abstract] [Full Text] [PDF]


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BloodHome page
B. D. Smolich, H. A. Yuen, K. A. West, F. J. Giles, M. Albitar, and J. M. Cherrington
The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts
Blood, March 1, 2001; 97(5): 1413 - 1421.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
R. M. Shaheen, W. W. Tseng, D. W. Davis, W. Liu, N. Reinmuth, R. Vellagas, A. A. Wieczorek, Y. Ogura, D. J. McConkey, K. E. Drazan, et al.
Tyrosine Kinase Inhibition of Multiple Angiogenic Growth Factor Receptors Improves Survival in Mice Bearing Colon Cancer Liver Metastases by Inhibition of Endothelial Cell Survival Mechanisms
Cancer Res., February 1, 2001; 61(4): 1464 - 1468.
[Abstract] [Full Text]


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Clin. Cancer Res.Home page
D. B. Mendel, R. E. Schreck, D. C. West, G. Li, L. M. Strawn, S. S. Tanciongco, S. Vasile, L. K. Shawver, and J. M. Cherrington
The Angiogenesis Inhibitor SU5416 Has Long-lasting Effects on Vascular Endothelial Growth Factor Receptor Phosphorylation and Function
Clin. Cancer Res., December 1, 2000; 6(12): 4848 - 4858.
[Abstract] [Full Text]




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