AEE788 is a multitargeted human epidermal receptor (HER) 1/2 and vascular endothelial growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited with IC50s of 11 and 220 nM, respectively. It efficiently inhibited growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h, a phenomenon correlating with the antitumor efficacy of intermittent treatment schedules. It also inhibits VEGF-induced angiogenesis in a murine implant model. It has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters. |
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InChI=1S/C6H12F2N2O2/c7-4(8)6(10,5(11)12)2-1-3-9/h4H,1-3,9-10H2,(H,11,12) |
VLCYCQAOQCDTCN-UHFFFAOYSA-N |
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Bronsted base
A molecular entity capable of accepting a hydron from a donor (Bronsted acid).
(via organic amino compound )
Bronsted acid
A molecular entity capable of donating a hydron to an acceptor (Bronsted base).
(via oxoacid )
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trypanocidal drug
A drug used to treat or prevent infections caused by protozoal organisms belonging to the suborder Trypanosomatida.
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trypanocidal drug
A drug used to treat or prevent infections caused by protozoal organisms belonging to the suborder Trypanosomatida.
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View more via ChEBI Ontology
2,5-diamino-2-(difluoromethyl)pentanoic acid
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2-(difluoromethyl)ornithine
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alpha-(Difluoromethyl)-DL-ornithine
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DrugCentral
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α-difluoromethylornithine
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ChemIDplus
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ALPHA-DIFLUOROMETHYLORNITHINE
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PDBeChem
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DFMO
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ChemIDplus
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DL-Ornithine, 2-(difluoromethyl)-
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KEGG COMPOUND
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Eflornithine
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KEGG COMPOUND
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990
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DrugCentral
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C07997
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KEGG COMPOUND
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D07883
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KEGG DRUG
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DB03856
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DrugBank
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DMO
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PDBeChem
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Eflornithine
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Wikipedia
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View more database links |
2250529
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Beilstein Registry Number
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ChemIDplus
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2250529
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Reaxys Registry Number
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Reaxys
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67037-37-0
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CAS Registry Number
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ChemIDplus
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70052-12-9
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CAS Registry Number
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ChemIDplus
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16541214
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PubMed citation
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Europe PMC
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23771434
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PubMed citation
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Europe PMC
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24144414
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PubMed citation
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Europe PMC
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