204005-46-9 | SU5416

Packsize	Purity	Availability	Price	Discounted Price
1mg	98%	in stock	$8.00	$6.00
5mg	98%	in stock	$18.00	$13.00
10mg	98%	in stock	$26.00	$18.00
50mg	98%	in stock	$68.00	$48.00
1g	≥98% (HPLC)	in stock	$1,007.00	$705.00

Description

• Catalog Number: AB05096
• Chemical Name: SU5416
• CAS Number: 204005-46-9
• Molecular Formula: C15H14N2O
• Molecular Weight: 238.2845
• MDL Number: MFCD09763655
• SMILES: O=C1Nc2c(C1=Cc1[nH]c(cc1C)C)cccc2
• NSC Number: 696819

Computed Properties

• Complexity: 377
• Covalently-Bonded Unit Count: 1
• Defined Bond Stereocenter Count: 1
• Heavy Atom Count: 18
• Hydrogen Bond Acceptor Count: 1
• Hydrogen Bond Donor Count: 2
• Rotatable Bond Count: 1
• XLogP3: 2.5

Literature

• Tumor-promoting and pro-angiogenic effects of roxarsone via VEGFR2/PLCγ/PKC signaling.

  Chemico-biological interactions 20180825

• Why are most phospholipidosis inducers also hERG blockers?

  Archives of toxicology 20171201

• The aryl hydrocarbon receptor is required for induction of p21cip1/waf1 expression and growth inhibition by SU5416 in hepatoma cells.

  Oncotarget 20170411

• Bromodomain-Containing Protein 4: The Epigenetic Origin of Pulmonary Arterial Hypertension.

  Circulation research 20150828

• Caveolin-1 is a negative regulator of NADPH oxidase-derived reactive oxygen species.

  Free radical biology & medicine 20140801

• NADPH oxidase 4 is expressed in pulmonary artery adventitia and contributes to hypertensive vascular remodeling.

  Arteriosclerosis, thrombosis, and vascular biology 20140801

• Identification of potent Yes1 kinase inhibitors using a library screening approach.

  Bioorganic & medicinal chemistry letters 20130801

• A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

  The Biochemical journal 20130415

• Resveratrol ameliorates high-glucose-induced hyperpermeability mediated by caveolae via VEGF/KDR pathway.

  Genes & nutrition 20130301

• Vitamin D improves the angiogenic properties of endothelial progenitor cells.

  American journal of physiology. Cell physiology 20121101

• Leptin induces tube formation in first-trimester extravillous trophoblast cells.

  European journal of obstetrics, gynecology, and reproductive biology 20120901

• Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.

  Bioorganic & medicinal chemistry 20120715

• VEGF regulates antidepressant effects of lamotrigine.

  European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology 20120601

• N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.

  Bioorganic & medicinal chemistry 20120401

• Study of differences in the VEGFR2 inhibitory activities between semaxanib and SU5205 using 3D-QSAR, docking, and molecular dynamics simulations.

  Journal of molecular graphics & modelling 20120201

• N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.

  Bioorganic & medicinal chemistry 20120115

• Inhibitory effects of SU5416, a selective vascular endothelial growth factor receptor tyrosine kinase inhibitor, on experimental corneal neovascularization.

  Ophthalmic research 20120101

• Normalization of the lymph node T cell stromal microenvironment in lpr/lpr mice is associated with SU5416-induced reduction in autoantibodies.

  PloS one 20120101

• The soluble guanylate cyclase stimulator riociguat ameliorates pulmonary hypertension induced by hypoxia and SU5416 in rats.

  PloS one 20120101

• SU5416, a VEGF receptor inhibitor and ligand of the AHR, represents a new alternative for immunomodulation.

  PloS one 20120101

• Unexpected neuronal protection of SU5416 against 1-Methyl-4-phenylpyridinium ion-induced toxicity via inhibiting neuronal nitric oxide synthase.

  PloS one 20120101

• Emerging therapies targeting tumor vasculature in multiple myeloma and other hematologic and solid malignancies.

  Current cancer drug targets 20111101

• Clinical experience with antiangiogenic therapy in leukemia.

  Current cancer drug targets 20111101

• Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

  Nature biotechnology 20111101

• [The effects of VEGF-R inhibitor on podocytopathy of rats with type I diabetic nephropathy].

  Xi bao yu fen zi mian yi xue za zhi = Chinese journal of cellular and molecular immunology 20110901

• Semaphorin-PlexinD1 signaling limits angiogenic potential via the VEGF decoy receptor sFlt1.

  Developmental cell 20110816

• SU5416 and EGCG work synergistically and inhibit angiogenic and survival factors and induce cell cycle arrest to promote apoptosis in human malignant neuroblastoma SH-SY5Y and SK-N-BE2 cells.

  Neurochemical research 20110801

• Peptide-directed highly selective targeting of pulmonary arterial hypertension.

  The American journal of pathology 20110601

• Virtual screening and further development of novel ALK inhibitors.

  Bioorganic & medicinal chemistry 20110515

• Androgen stimulates endothelial cell proliferation via an androgen receptor/VEGF/cyclin A-mediated mechanism.

  American journal of physiology. Heart and circulatory physiology 20110401

• Suppression of choroidal neovascularization by intravitreal injection of liposomal SU5416.

  Archives of ophthalmology (Chicago, Ill. : 1960) 20110301

• The effects of antiangiogenic compound SU5416 in a rat model of pulmonary arterial hypertension.

  Respiration; international review of thoracic diseases 20110101

• SU5416 induces premature senescence in endothelial progenitor cells from patients with age-related macular degeneration.

  Molecular vision 20110101

• A novel xenograft model in zebrafish for high-resolution investigating dynamics of neovascularization in tumors.

  PloS one 20110101

• Angiogenesis but not neurogenesis is critical for normal learning and memory acquisition.

  Neuroscience 20101124

• Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633.

  Cancer letters 20101001

• Adrenergic receptor blockade reverses right heart remodeling and dysfunction in pulmonary hypertensive rats.

  American journal of respiratory and critical care medicine 20100901

• Anti-vascular endothelial growth factor treatment in combination with chemotherapy delays hematopoietic recovery due to decreased proliferation of bone marrow hematopoietic progenitor cells.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20100901

• Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.

  Bioorganic & medicinal chemistry 20100715

• Novel pyrazole derivatives: synthesis and evaluation of anti-angiogenic activity.

  Bioorganic & medicinal chemistry 20100615

• The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines.

  Bioorganic & medicinal chemistry letters 20100515

• Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.

  Bioorganic & medicinal chemistry 20100515

• TSU-16, (Z)-3-[(2,4-dimethylpyrrol-5-yl)methylidenyl]-2-indolinone, is a potent activator of aryl hydrocarbon receptor and increases CYP1A1 and CYP1A2 expression in human hepatocytes.

  Chemico-biological interactions 20100415

• CREB activation mediates VEGF-A's protection of neurons and cerebral vascular endothelial cells.

  Journal of neurochemistry 20100401

• Vascular endothelial growth factor is involved in mediating increased de novo hippocampal neurogenesis in response to traumatic brain injury.

  Journal of neurotrauma 20100301

• Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.

  Journal of medicinal chemistry 20100225

• Stimulation of sphingosine 1-phosphate signaling as an alveolar cell survival strategy in emphysema.

  American journal of respiratory and critical care medicine 20100215

• Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.

  Bioorganic & medicinal chemistry 20100215

• Vascular endothelial growth factor receptor-2 inhibition promotes cell death and limits endothelial cell proliferation in a neonatal rodent model of stroke.

  Stroke 20100201

• ERK1/2-dependent vascular endothelial growth factor signaling sustains cyst growth in polycystin-2 defective mice.

  Gastroenterology 20100101

• Tumor secretion of VEGF induces endothelial cells to suppress T cell functions through the production of PGE2.

  Journal of immunotherapy (Hagerstown, Md. : 1997) 20100101

• Synthesis and radiopharmacological investigation of 3-[4'-[(18)F]fluorobenzylidene]indolin-2-one as possible tyrosine kinase inhibitor.

  Bioorganic & medicinal chemistry 20091115

• Reduction in endothelial tip cell filopodia corresponds to reduced intravitreous but not intraretinal vascularization in a model of ROP.

  Experimental eye research 20091101

• Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.

  Bioorganic & medicinal chemistry 20091015

• Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

  Nature chemical biology 20091001

• Vascular endothelial growth factor receptor inhibitor enhances dietary salt-induced hypertension in Sprague-Dawley rats.

  American journal of physiology. Regulatory, integrative and comparative physiology 20090701

• Genetic evidence for a noncanonical function of seryl-tRNA synthetase in vascular development.

  Circulation research 20090605

• VEGF and angiogenesis in acute and chronic MOG((35-55)) peptide induced EAE.

  Journal of neuroimmunology 20090430

• Oral administration of pyrrolidine dithiocarbamate (PDTC) inhibits VEGF expression, tumor angiogenesis, and growth of breast cancer in female mice.

  Cancer biology & therapy 20090315

• VEGFR1 receptor tyrosine kinase localization to the Golgi apparatus is calcium-dependent.

  Experimental cell research 20090310

• Phase I study of SU5416, a small molecule inhibitor of the vascular endothelial growth factor receptor (VEGFR) in refractory pediatric central nervous system tumors.

  Pediatric blood & cancer 20090201

• VEGFR-2 antagonist SU5416 attenuates bleomycin-induced pulmonary fibrosis in mice.

  International immunopharmacology 20090101

• Ligation or cross-linking of CD40 has different effects on AGS gastric cancer cells.

  Cellular immunology 20090101

• Antiangiogenic cancer therapy using tumor vasculature-targeted liposomes encapsulating 3-(3,5-dimethyl-1H-pyrrol-2-ylmethylene)-1,3-dihydro-indol-2-one, SU5416.

  Cancer letters 20081108

• Antiangiogenic and anticolorectal cancer effects of metronomic irinotecan chemotherapy alone and in combination with semaxinib.

  British journal of cancer 20080520

• Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.

  Bioorganic & medicinal chemistry 20080515

• Combination of vascular endothelial growth factor receptor/platelet-derived growth factor receptor inhibition markedly improves radiation tumor therapy.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20080401

• Impaired VEGF and nitric oxide signaling after nitrofen exposure in rat fetal lung explants.

  American journal of physiology. Lung cellular and molecular physiology 20080101

• Should tumor VEGF expression influence decisions on combining low-dose chemotherapy with antiangiogenic therapy? Preclinical modeling in ovarian cancer.

  Journal of translational medicine 20080101

• Targeting the vascular endothelial growth factor system to prevent ovarian hyperstimulation syndrome.

  Human reproduction update 20080101

• Inhibition of choroidal neovascularization by blocking vascular endothelial growth factor receptor tyrosine kinase.

  Japanese journal of ophthalmology 20080101

• Development of an intravenous formulation of SU010382 (prodrug of SU5416, an anti-angiogenesis agent).

  PDA journal of pharmaceutical science and technology 20080101

• VEGF modulation of retinal pigment epithelium resistance.

  Experimental eye research 20071201

• Role of NADPH oxidase and ANG II in diabetes-induced retinal leukostasis.

  American journal of physiology. Regulatory, integrative and comparative physiology 20071001

• Effect of chemical stabilizers of hypoxia-inducible factors on early lung development.

  American journal of physiology. Lung cellular and molecular physiology 20070901

• Semaxinib (SU5416) as a therapeutic agent targeting oncogenic Kit mutants resistant to imatinib mesylate.

  Oncogene 20070531

• A Phase II study of SU5416 in patients with advanced or recurrent head and neck cancers.

  Investigational new drugs 20070401

• Rho kinase-mediated vasoconstriction is important in severe occlusive pulmonary arterial hypertension in rats.

  Circulation research 20070330

• Synthesis and evaluation of prodrugs for anti-angiogenic pyrrolylmethylidenyl oxindoles.

  Bioorganic & medicinal chemistry letters 20070315

• Effects of vascular endothelial growth factor receptor inhibitor SU5416 and prostacyclin on murine lung metastasis.

  Anti-cancer drugs 20070301

• A phase II, pharmacokinetic, and biologic study of semaxanib and thalidomide in patients with metastatic melanoma.

  Cancer chemotherapy and pharmacology 20070201

• [Clinical importance of angiogenesis and angiogenic factors in oncohematology].

  Wiadomosci lekarskie (Warsaw, Poland : 1960) 20070101

• Downregulation of VEGF-A, STAT5 and AKT in acute myeloid leukemia blasts of patients treated with SU5416.

  Leukemia & lymphoma 20061201

• Blockade of vascular endothelial growth factor signaling ameliorates diabetic albuminuria in mice.

  Journal of the American Society of Nephrology : JASN 20061101

• Simvastatin causes endothelial cell apoptosis and attenuates severe pulmonary hypertension.

  American journal of physiology. Lung cellular and molecular physiology 20061001

• An orally administered multitarget tyrosine kinase inhibitor, SU11248, is a novel potent inhibitor of thyroid oncogenic RET/papillary thyroid cancer kinases.

  The Journal of clinical endocrinology and metabolism 20061001

• Structure-activity-relationship studies of conformationally restricted analogs of combretastatin A-4 derived from SU5416.

  Bioorganic & medicinal chemistry 20061001

• Inhibition of RET tyrosine kinase by SU5416.

  Journal of molecular endocrinology 20061001

• [Recent advances in the study of pharmacological activities and solid-phase synthesis of indoles and their analogues].

  Yao xue xue bao = Acta pharmaceutica Sinica 20060801

• Antiangiogenic combination tumor therapy blocking alpha(v)-integrins and VEGF-receptor-2 increases therapeutic effects in vivo.

  International journal of cancer 20060715

• A phase I study with oral SU5416 in patients with advanced solid tumors: a drug inducing its clearance.

  Investigational new drugs 20060701

• VEGF-C promotes survival in podocytes.

  American journal of physiology. Renal physiology 20060701

• Vascular endothelial growth factor and hepatocyte regeneration in acetaminophen toxicity.

  American journal of physiology. Gastrointestinal and liver physiology 20060701

• Anti-angiogenic and anti-HER therapy.

  Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 20060701

• Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.

  Journal of medicinal chemistry 20060601

• Microsphere-based protease assays and screening application for lethal factor and factor Xa.

  Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501

• Phase I/pilot study of SU5416 (semaxinib) in combination with irinotecan/bolus 5-FU/LV (IFL) in patients with metastatic colorectal cancer.

  American journal of clinical oncology 20060401

• Distribution, metabolism, and excretion of the anti-angiogenic compound SU5416.

  Toxicology in vitro : an international journal published in association with BIBRA 20060301

• Emerging Flt3 kinase inhibitors in the treatment of leukaemia.

  Expert opinion on emerging drugs 20060301

• A Phase I study of escalating doses of the tyrosine kinase inhibitor semaxanib (SU5416) in combination with irinotecan in patients with advanced colorectal carcinoma.

  Japanese journal of clinical oncology 20060201

• Clinical implications for vascular endothelial growth factor in the lung: friend or foe?

  Respiratory research 20060101

• Conformationally restricted analogs of Combretastatin A-4 derived from SU5416.

  Bioorganic & medicinal chemistry letters 20051215

• Enhancing the therapeutic responsiveness of photodynamic therapy with the antiangiogenic agents SU5416 and SU6668 in murine nasopharyngeal carcinoma models.

  Cancer chemotherapy and pharmacology 20051201

• Nerve growth factor-induced migration of endothelial cells.

  The Journal of pharmacology and experimental therapeutics 20051201

• A Phase I study of the angiogenesis inhibitor SU5416 (semaxanib) in solid tumours, incorporating dynamic contrast MR pharmacodynamic end points.

  British journal of cancer 20051017

• Functional CT for quantifying tumor perfusion in antiangiogenic therapy in a rat model.

  Radiology 20051001

• Indolin-2-ones with high in vivo efficacy in a model for multiple sclerosis.

  Journal of medicinal chemistry 20050825

• Initial apoptosis is followed by increased proliferation of apoptosis-resistant endothelial cells.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20050701

• In vitro procoagulant activity induced in endothelial cells by chemotherapy and antiangiogenic drug combinations: modulation by lower-dose chemotherapy.

  Cancer research 20050615

• [Potential pharmacological treatments for diabetic retinopathy].

  Nihon rinsho. Japanese journal of clinical medicine 20050601

• [Medications for diabetic macular edema].

  Nihon rinsho. Japanese journal of clinical medicine 20050601

• Vascular endothelial growth factor: a therapeutic target for tumors of the Ewing's sarcoma family.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20050315

• C-kit as a target in the treatment of acute myelogenous leukemia.

  Current hematology reports 20050101

• Differential roles of vascular endothelial growth factor receptors 1 and 2 in dendritic cell differentiation.

  Journal of immunology (Baltimore, Md. : 1950) 20050101

• Emphysema: an autoimmune vascular disease?

  Proceedings of the American Thoracic Society 20050101

• Triple combination of irradiation, chemotherapy (pemetrexed), and VEGFR inhibition (SU5416) in human endothelial and tumor cells.

  International journal of radiation oncology, biology, physics 20041115

• SU5416 inhibited VEGF and HIF-1alpha expression through the PI3K/AKT/p70S6K1 signaling pathway.

  Biochemical and biophysical research communications 20041112

• c-Myc interacts with hypoxia to induce angiogenesis in vivo by a vascular endothelial growth factor-dependent mechanism.

  Cancer research 20040915

• Antiangiogenic versus cytotoxic therapeutic approaches to human pancreas cancer: an experimental study with a vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor and gemcitabine.

  European journal of pharmacology 20040913

• Vascular endothelial growth factor in diabetes induced early retinal abnormalities.

  Diabetes research and clinical practice 20040901

• Phase II study of the antiangiogenic agent SU5416 in patients with advanced soft tissue sarcomas.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20040901

• SU5416 is a potent inhibitor of hepatocyte growth factor receptor (c-Met) and blocks HGF-induced invasiveness of human HepG2 hepatoma cells.

  Journal of hepatology 20040801

• Effects of SU5416, a small molecule tyrosine kinase receptor inhibitor, on FLT3 expression and phosphorylation in patients with refractory acute myeloid leukemia.

  Leukemia research 20040701

• Phase II study of the Flk-1 tyrosine kinase inhibitor SU5416 in advanced melanoma.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20040615

• Determination of SU5416, a novel angiogenesis inhibitor, in human plasma by liquid chromatography.

  Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20040605

• The c-Cbl/CD2AP complex regulates VEGF-induced endocytosis and degradation of Flt-1 (VEGFR-1).

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20040501

• The vascular endothelial growth factor (VEGF) receptor Flt-1 (VEGFR-1) modulates Flk-1 (VEGFR-2) signaling during blood vessel formation.

  The American journal of pathology 20040501

• [Lung cancer: molecular targeting therapy].

  Nihon Kokyuki Gakkai zasshi = the journal of the Japanese Respiratory Society 20040501

• New cancer therapeutics: target-specific in, cytotoxics out?

  Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy 20040401

• Anti-vascular tumor therapy: recent advances, pitfalls and clinical perspectives.

  Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy 20040401

• N-acetylcysteine treatment protects against VEGF-receptor blockade-related emphysema.

  COPD 20040401

• Antiangiogenic therapy for von Hippel-Lindau disease.

  JAMA 20040225

• Combined inhibition of VEGF and PDGF signaling enforces tumor vessel regression by interfering with pericyte-mediated endothelial cell survival mechanisms.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20040201

• Plasma and cerebrospinal fluid pharmacokinetics of SU5416 after intravenous administration in nonhuman primates.

  Cancer chemotherapy and pharmacology 20040101

• Phase II study of SU5416, a small molecule vascular endothelial growth factor tyrosine kinase receptor inhibitor, in patients with refractory multiple myeloma.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20040101

• Complete radiological and metabolic response of metastatic renal cell carcinoma to SU5416 (semaxanib) in a patient with probable von Hippel-Lindau syndrome.

  Urologic oncology 20040101

• Combined therapy with direct and indirect angiogenesis inhibition results in enhanced antiangiogenic and antitumor effects.

  Cancer research 20031215

• SU5416 plus interferon alpha in advanced renal cell carcinoma: a phase II California Cancer Consortium Study with biological and imaging correlates of angiogenesis inhibition.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20031015

• Human NADPH-cytochrome p450 reductase overexpression does not enhance the aerobic cytotoxicity of doxorubicin in human breast cancer cell lines.

  Cancer research 20031015

• The antiangiogenic agent SU5416 down-regulates phorbol ester-mediated induction of cyclooxygenase 2 expression by inhibiting nicotinamide adenine dinucleotide phosphate oxidase activity.

  Cancer research 20031015

• Suppression of experimental choroidal neovascularization utilizing KDR selective receptor tyrosine kinase inhibitor.

  Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie 20030901

• SU5416, a small molecule tyrosine kinase receptor inhibitor, has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromes.

  Blood 20030801

• Research retreat: Pfizer eliminates Sugen, shrinks cancer infrastructure.

  Journal of the National Cancer Institute 20030716

• Oxidative stress and apoptosis interact and cause emphysema due to vascular endothelial growth factor receptor blockade.

  American journal of respiratory cell and molecular biology 20030701

• Treatment of von Hippel-Lindau retinal hemangioblastoma by the vascular endothelial growth factor receptor inhibitor SU5416 is more effective for associated macular edema than for hemangioblastomas.

  American journal of ophthalmology 20030701

• SU5416 and SU6668 attenuate the angiogenic effects of radiation-induced tumor cell growth factor production and amplify the direct anti-endothelial action of radiation in vitro.

  Cancer research 20030701

• SU5416 selectively impairs angiogenesis to induce prostate cancer-specific apoptosis.

  Molecular cancer therapeutics 20030701

• Pharmacodynamic-mediated effects of the angiogenesis inhibitor SU5416 on the tumor disposition of temozolomide in subcutaneous and intracerebral glioma xenograft models.

  The Journal of pharmacology and experimental therapeutics 20030601

• Potential role of platelets in endothelial damage observed during treatment with cisplatin, gemcitabine, and the angiogenesis inhibitor SU5416.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20030601

• Potential inhibitors of angiogenesis. Part I: 3-(imidazol-4(5)-ylmethylene)indolin-2-ones.

  Journal of enzyme inhibition and medicinal chemistry 20030601

• Potential inhibitors of angiogenesis. Part II: 3-(azolylmethylene)-2,3-dihydrobenzo[b]furan-2-ones.

  Journal of enzyme inhibition and medicinal chemistry 20030601

• Vascular endothelial growth factor (VEGF) receptor-2 signaling mediates VEGF-C(deltaNdeltaC)- and VEGF-A-induced angiogenesis in vitro.

  Experimental cell research 20030501

• Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors.

  The Journal of clinical investigation 20030501

• Efficacy and toxicity of the angiogenesis inhibitor SU5416 as a single agent in patients with advanced renal cell carcinoma, melanoma, and soft tissue sarcoma.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20030501

• Phase II study of SU5416--a small-molecule, vascular endothelial growth factor tyrosine-kinase receptor inhibitor--in patients with refractory myeloproliferative diseases.

  Cancer 20030415

• [From molecular biology to new treatment approaches to colorectal cancer: basic research, experimental trials and surgical implications].

  Il Giornale di chirurgia 20030401

• Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.

  Journal of medicinal chemistry 20030327

• Effect of angiogenesis inhibitors on oestrogen-mediated endometrial endothelial cell proliferation in the ovariectomized mouse.

  Reproduction (Cambridge, England) 20030301

• Improved effect of an antiangiogenic tyrosine kinase inhibitor (SU5416) by combinations with fractionated radiotherapy or low molecular weight heparin.

  Neoplasia (New York, N.Y.) 20030301

• [Perspectives on the oncologist pharmacopoeia].

  Bulletin du cancer 20030101

• Expression profiling of blood samples from an SU5416 Phase III metastatic colorectal cancer clinical trial: a novel strategy for biomarker identification.

  BMC cancer 20030101

• Flt3 in acute myelogenous leukemia: biology, prognosis, and therapeutic implications.

  Medical oncology (Northwood, London, England) 20030101

• Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.

  Journal of medicinal chemistry 20021219

• Synthetic lethality: killing cancer with cancer.

  Journal of the National Cancer Institute 20021120

• Zebrafish: a preclinical model for drug screening.

  Assay and drug development technologies 20021101

• SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase.

  Blood 20021015

• Inhibitors of the vascular endothelial growth factor receptor.

  Hematology/oncology clinics of North America 20021001

• New drugs in acute myeloid leukemia.

  Current oncology reports 20020901

• Rapid and durable recovery of visual function in a patient with von hippel-lindau syndrome after systemic therapy with vascular endothelial growth factor receptor inhibitor su5416.

  Ophthalmology 20020901

• Results of a Phase I dose-escalating study of the antiangiogenic agent, SU5416, in patients with advanced malignancies.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20020901

• Targeting vascular endothelial growth factor in colorectal cancer.

  Oncology (Williston Park, N.Y.) 20020801

• A novel dihydroxanthenone, AGI-B4 with inhibition of VEGF-induced endothelial cell growth.

  The Journal of antibiotics 20020701

• Vascular endothelial growth factor-mediated angiogenesis inhibition and postoperative wound healing in rats.

  The Journal of surgical research 20020601

• Orthogonal polarisation spectral imaging as a new tool for the assessment of antivascular tumour treatment in vivo: a validation study.

  British journal of cancer 20020520

• CHS 828 inhibits neuroblastoma growth in mice alone and in combination with antiangiogenic drugs.

  Pediatric research 20020501

• Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.

  The Journal of biological chemistry 20020419

• Unexpected serious toxicity with chemotherapy and antiangiogenic combinations: time to take stock!

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20020315

• Dose-finding and pharmacokinetic study of cisplatin, gemcitabine, and SU5416 in patients with solid tumors.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20020315

• Inhibition of KIT tyrosine kinase activity: a novel molecular approach to the treatment of KIT-positive malignancies.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20020315

• Antiangiogenic effect by SU5416 is partly attributable to inhibition of Flt-1 receptor signaling.

  Molecular cancer therapeutics 20020301

• SU5416 delays wound healing through inhibition of TGF-beta 1 activation.

  Cancer biology & therapy 20020101

• New chemotherapeutic agents: update of major chemoradiation trials in solid tumors.

  Oncology 20020101

• Comparative study of isoflavone, quinoxaline and oxindole families of anti-angiogenic agents.

  Angiogenesis 20020101

• Combining antiangiogenic agents with metronomic chemotherapy enhances efficacy against late-stage pancreatic islet carcinomas in mice.

  Cold Spring Harbor symposia on quantitative biology 20020101

• Importance of vascular endothelial growth factor A in the progression of experimental neuroblastoma.

  Angiogenesis 20020101

• Sequential tumor biopsies in early phase clinical trials of anticancer agents for pharmacodynamic evaluation.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20011001

• Flk-1 specific kinase inhibitor (SU5416) inhibited the growth of GS-9L glioma in rat brain and prolonged the survival.

  The Kobe journal of medical sciences 20010801

• Simultaneous determination of SU5416 and its phase I and phase II metabolites in rat and dog plasma by LC/MS/MS.

  Journal of pharmaceutical and biomedical analysis 20010701

• Stable remission after administration of the receptor tyrosine kinase inhibitor SU5416 in a patient with refractory acute myeloid leukemia.

  Blood 20010701

• Magnetic resonance imaging of ethyl-nitrosourea-induced rat gliomas: a model for experimental therapeutics of low-grade gliomas.

  Journal of neuro-oncology 20010701

• Indolinone tyrosine kinase inhibitors block Kit activation and growth of small cell lung cancer cells.

  Cancer research 20010501

• Nonvascular role for VEGF: VEGFR-1, 2 activity is critical for neural retinal development.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20010501

• [Tumor angiogenesis and tumor angiogenesis inhibitors].

  Gan to kagaku ryoho. Cancer & chemotherapy 20010501

• 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 20010301

• The vascular endothelial growth factor (VEGF) signaling pathway: a therapeutic target in patients with hematologic malignancies.

  The oncologist 20010101

• Endothelial survival factors as targets for antineoplastic therapy.

  Cancer journal (Sudbury, Mass.) 20010101

• Role of angiogenesis inhibitors in acute myeloid leukemia.

  Cancer journal (Sudbury, Mass.) 20010101

• Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.

  Journal of medicinal chemistry 20000713

• New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.

  Journal of medicinal chemistry 20000615

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