497839-62-0 | AEE788

Packsize	Purity	Availability	Price	Discounted Price
1mg	98%	in stock	$49.00	$35.00
5mg	98%	in stock	$145.00	$101.00
10mg	98%	in stock	$218.00	$152.00
50mg	98%	in stock	$865.00	$606.00

Description

• Catalog Number: AD23938
• Chemical Name: AEE788
• CAS Number: 497839-62-0
• Molecular Formula: C27H32N6
• Molecular Weight: 440.5832
• MDL Number: MFCD11100351
• SMILES: CCN1CCN(CC1)Cc1ccc(cc1)c1cc2c([nH]1)ncnc2N[C@@H](c1ccccc1)C

Computed Properties

• Complexity: 579
• Covalently-Bonded Unit Count: 1
• Defined Atom Stereocenter Count: 1
• Heavy Atom Count: 33
• Hydrogen Bond Acceptor Count: 5
• Hydrogen Bond Donor Count: 2
• Rotatable Bond Count: 7
• XLogP3: 4.6

Literature

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

  Bioorganic & medicinal chemistry letters 20130801

• Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.

  Journal of medicinal chemistry 20121227

• Using pharmacokinetic and pharmacodynamic data in early decision making regarding drug development: a phase I clinical trial evaluating tyrosine kinase inhibitor, AEE788.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20121115

• AEE788 potentiates celecoxib-induced growth inhibition and apoptosis in human colon cancer cells.

  Life sciences 20121022

• Effects of epidermal growth factor receptor blockade on ependymoma stem cells in vitro and in orthotopic mouse models.

  International journal of cancer 20120901

• Phase I study of AEE788, a novel multitarget inhibitor of ErbB- and VEGF-receptor-family tyrosine kinases, in recurrent glioblastoma patients.

  Cancer chemotherapy and pharmacology 20120601

• Pharmacokinetic drug interaction between AEE788 and RAD001 causing thrombocytopenia in patients with glioblastoma.

  Cancer chemotherapy and pharmacology 20120101

• Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines.

  European journal of medicinal chemistry 20111201

• Rapid and accurate ranking of binding affinities of epidermal growth factor receptor sequences with selected lung cancer drugs.

  Journal of the Royal Society, Interface 20110807

• The anti-proliferative side effects of AEE788, a tyrosine kinase inhibitor blocking both EGF- and VEGF-receptor, are liver-size-dependent after partial hepatectomy in rats.

  Investigational new drugs 20110801

• Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors.

  Bioorganic & medicinal chemistry letters 20110801

• Critical analysis of simultaneous blockage of histone deacetylase and multiple receptor tyrosine kinase in the treatment of prostate cancer.

  The Prostate 20110515

• Combined targeting of the VEGFr/EGFr and the mammalian target of rapamycin (mTOR) signaling pathway delays cell cycle progression and alters adhesion behavior of prostate carcinoma cells.

  Cancer letters 20110201

• Molecular targeting of prostate cancer cells by a triple drug combination down-regulates integrin driven adhesion processes, delays cell cycle progression and interferes with the cdk-cyclin axis.

  BMC cancer 20110101

• AEE788 is a vascular endothelial growth factor receptor tyrosine kinase inhibitor with antiproliferative and proapoptotic effects in acute myeloid leukemia.

  Experimental hematology 20100801

• The combination of multiple receptor tyrosine kinase inhibitor and mammalian target of rapamycin inhibitor overcomes erlotinib resistance in lung cancer cell lines through c-Met inhibition.

  Molecular cancer research : MCR 20100801

• EGFR/HER2 inhibitor AEE788 increases ER-mediated transcription in HER2/ER-positive breast cancer cells but functions synergistically with endocrine therapy.

  British journal of cancer 20100413

• Effect of AEE788 and/or Celecoxib on colon cancer cell morphology using advanced microscopic techniques.

  Micron (Oxford, England : 1993) 20100401

• Effects of combined valproic acid and the epidermal growth factor/vascular endothelial growth factor receptor tyrosine kinase inhibitor AEE788 on renal cell carcinoma cell lines in vitro.

  BJU international 20100201

• Effect and risk of AEE788, a dual tyrosine kinase inhibitor, on regeneration in a rat liver resection model.

  European surgical research. Europaische chirurgische Forschung. Recherches chirurgicales europeennes 20100101

• Targeting angiogenesis in hepatocellular carcinoma: focus on VEGF and bevacizumab.

  Expert review of anticancer therapy 20090401

• Combining the receptor tyrosine kinase inhibitor AEE788 and the mammalian target of rapamycin (mTOR) inhibitor RAD001 strongly inhibits adhesion and growth of renal cell carcinoma cells.

  BMC cancer 20090101

• EGFR-dependent migration of glial cells is mediated by reorganisation of N-cadherin.

  Journal of cell science 20081215

• The dual EGF/VEGF receptor tyrosine kinase inhibitor AEE788 inhibits growth of human hepatocellular carcinoma xenografts in nude mice.

  International journal of oncology 20081001

• [Preclinical studies on the influence of the tyrosine kinase inhibitor AEE788 on malignant properties of renal cell carcinoma cells].

  Der Urologe. Ausg. A 20080901

• Targeting the EGFR, VEGFR, and PDGFR on colon cancer cells and stromal cells is required for therapy.

  Clinical & experimental metastasis 20080101

• Inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation on tumor-associated endothelial cells leads to treatment of orthotopic human colon cancer in nude mice.

  Neoplasia (New York, N.Y.) 20071201

• Study of two tyrosine kinase inhibitors on growth and signal transduction in polycythemia vera.

  Experimental hematology 20071101

• Expression of epidermal growth factor (EGF)/transforming growth factor-alpha by human lung cancer cells determines their response to EGF receptor tyrosine kinase inhibition in the lungs of mice.

  Molecular cancer therapeutics 20071001

• Hypoxia modulation and radiosensitization by the novel dual EGFR and VEGFR inhibitor AEE788 in spontaneous and related allograft tumor models.

  Molecular cancer therapeutics 20070901

• Differential effects of cetuximab and AEE 788 on epidermal growth factor receptor (EGF-R) and vascular endothelial growth factor receptor (VEGF-R) in thyroid cancer cell lines.

  Endocrine 20070401

• The EGF receptor Hokey-Cokey.

  Cancer cell 20070301

• Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.

  Cancer cell 20070301

• Abrogation of MAPK and Akt signaling by AEE788 synergistically potentiates histone deacetylase inhibitor-induced apoptosis through reactive oxygen species generation.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20070215

• Combination of sublethal concentrations of epidermal growth factor receptor inhibitor and microtubule stabilizer induces apoptosis of glioblastoma cells.

  Molecular cancer therapeutics 20070201

• Metronomic chemotherapy enhances the efficacy of antivascular therapy in ovarian cancer.

  Cancer research 20070101

• Pharmacology of epidermal growth factor inhibitors.

  The International journal of biological markers 20070101

• Rationale and clinical results of multi-target treatments in oncology.

  The International journal of biological markers 20070101

• Concomitant inhibition of epidermal growth factor and vascular endothelial growth factor receptor tyrosine kinases reduces growth and metastasis of human salivary adenoid cystic carcinoma in an orthotopic nude mouse model.

  Molecular cancer therapeutics 20061101

• Epidermal growth factor receptor as a therapeutic target in human thyroid carcinoma: mutational and functional analysis.

  The Journal of clinical endocrinology and metabolism 20060901

• New molecular targeted therapies in thyroid cancer.

  Anti-cancer drugs 20060901

• Targeting receptor tyrosine kinase on lymphatic endothelial cells for the therapy of colon cancer lymph node metastasis.

  Neoplasia (New York, N.Y.) 20060901

• Novel targeted approaches to treating biliary tract cancer: the dual epidermal growth factor receptor and ErbB-2 tyrosine kinase inhibitor NVP-AEE788 is more efficient than the epidermal growth factor receptor inhibitors gefitinib and erlotinib.

  Anti-cancer drugs 20060801

• Dual epidermal growth factor receptor and vascular endothelial growth factor receptor inhibition with NVP-AEE788 for the treatment of aggressive follicular thyroid cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20060601

• Simultaneous inhibition of EGFR, VEGFR, and platelet-derived growth factor receptor signaling combined with gemcitabine produces therapy of human pancreatic carcinoma and prolongs survival in an orthotopic nude mouse model.

  Cancer research 20051115

• Dual inhibition of the epidermal growth factor and vascular endothelial growth factor phosphorylation for antivascular therapy of human prostate cancer in the prostate of nude mice.

  The Prostate 20051101

• Antivascular therapy for orthotopic human ovarian carcinoma through blockade of the vascular endothelial growth factor and epidermal growth factor receptors.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20050701

• Induction of apoptosis in tumor-associated endothelial cells and therapy of orthotopic human pancreatic carcinoma in nude mice.

  Neoplasia (New York, N.Y.) 20050701

• Antivascular therapy of human follicular thyroid cancer experimental bone metastasis by blockade of epidermal growth factor receptor and vascular growth factor receptor phosphorylation.

  Cancer research 20050601

• Dual inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation by AEE788 reduces growth and metastasis of human colon carcinoma in an orthotopic nude mouse model.

  Cancer research 20050501

• Targeted molecular therapy of anaplastic thyroid carcinoma with AEE788.

  Molecular cancer therapeutics 20050401

• AEE788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20050301

• Combination therapy of inhibitors of epidermal growth factor receptor/vascular endothelial growth factor receptor 2 (AEE788) and the mammalian target of rapamycin (RAD001) offers improved glioblastoma tumor growth inhibition.

  Molecular cancer therapeutics 20050101

• Tumor cell and endothelial cell therapy of oral cancer by dual tyrosine kinase receptor blockade.

  Cancer research 20041101

• AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.

  Cancer research 20040715