Home
Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassay Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
Polymers & Contract Manufacturing
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Products
Small Molecule Inhibitors and Antagonist
Bioactive Compounds and Agonist
Primary Antibodies
Catalog Peptides
Amino Acids Derivatives
Reagents
Fluorescent dyes
Intermediates
PCR
Proteasomes and Enzymes
Enzyme substrate
Nucleotides
Promotions
Customer Support
About Us
Site Map
Contact Us
Small Molecule Inhibitors and Antagonist
Anti-virus
Cell Cycle
DMPK/Tox
Endocrinology
Epigenetics
GPCR/G-protein
Mitogen-activated Protein Kinases (MAPK)
PI3K/Akt/mTOR
Proteases/Proteasome
Protein Tyrosine Kinases (PTK)
Stem Cells
TGF-Beta/Smad
Transporter
Others
Cat. No. Name Size Price Add Cart
KI1299AEE7885 mg$272
AEE78810 mg$512
AEE78825 mg$912
AEE78850 mg$1552

Chemical Characteristic

Product NameAEE788
SynonymsNVP-AEE788
CAS No.497839-62-0
Molecular Weight 440.58
FormulaC27H32N6
Chemical Name6-[4-[(4-Ethyl-1-piperazinyl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Smilesc1nc2c(c(n1)N[C@H](C)c1ccccc1)cc([nH]2)c1ccc(cc1)CN1CCN(CC1)CC
Chemical Structure

Biological activities

AEE788 is a novel multitargeted inhibitor of EGFR, ErbB2, KDR, and Flt-1 with IC50 values of 2, 6, 77 and 59 nM, respectively.[1] Cell treatment with AEE788 (1-5 µM) and HDAC inhibitors (LBH589 and LAQ824) in combination results in synergistic induction of apoptosis in non-small cell lung cancer (MV522, A549), ovarian cancer (SKOV-3), and leukemia (K562, Jurkat, and ML-1) cells and in OV202hp cisplatin-resistant human ovarian cancer cells.[2] In cutaneous SCC cells in vitro, AEE788 treatment leads to dose-dependent inhibition of EGFR and VEGFR-2 phosphorylation, growth inhibition, and induction of apoptosis. In mice injected with Colo16 cells, AEE788 (50 mg/kg) inhibits tumor growth by 54% at 21 days after the start of treatment compared with control mice. AEE788 (50 mg/kg) also inhibits phosphorylation of EGFR and VEGFR and induces apoptosis of tumor cells and tumor-associated endothelial cells.[3] In human colon carcinoma xenografts model, mice treated with the combination of AEE788 (50 mg/kg) and CPT-11 have significantly smaller tumors and complete inhibition of lymph node metastasis.[4]

Protocols

In vivo: AEE788 is stored at room temperature and diluted in DMSO before oral administration.[4]

References

[1] Traxler P, et al. AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2004, 64(14): 4931-4941.
[2] Yu C, et al. Abrogation of MAPK and Akt signaling by AEE788 synergistically potentiates histone deacetylase inhibitor-induced apoptosis through reactive oxygen species generation. Clin Cancer Res. 2007, 13(4): 1140-1148.
[3] Park YW, et al. AEE788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice. Clin Cancer Res. 2005, 11(5): 1963-1973.
[4] Yokoi K, et al. 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 Res. 2005, 65(9): 3716-3725.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.
KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
About
KareBayTM Biochem
Sitemap
Blog
Custom Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Biochemical Products
Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR
Contact Us
KareBayTM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852
Telephone
: 732-823-1545

Fax
: 732-823-1349
product@karebaybio.com
service@karebaybio.com
support@karebaybio.com
Follow Us
Follow Karebay on LinkedinFollow IMAGING on Twitter Google+ Facebook