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/C14H15N7/c15-13(16)9-1-5-11(6-2-9)19-21-20-12-7-3-10(4-8-12)14(17)18/h1-8H,(H3,15,16)(H3,17,18)(H,19,20) |
XNYZHCFCZNMTFY-UHFFFAOYSA-N |
NC(=N)c1ccc(NN=Nc2ccc(cc2)C(N)=N)cc1 |
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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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antiparasitic agent
A substance used to treat or prevent parasitic infections.
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
4,4'-triaz-1-ene-1,3-diyldibenzenecarboximidamide
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diminazène
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WHO MedNet
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diminazene
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ChemIDplus
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diminazeno
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ChemIDplus
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diminazenum
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ChemIDplus
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4,4'-(1-triazene-1,3-diyl)bis-benzenecarboximidamide
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ChemIDplus
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3153756
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Reaxys Registry Number
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Reaxys
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536-71-0
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CAS Registry Number
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KEGG COMPOUND
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536-71-0
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CAS Registry Number
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ChemIDplus
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5757660
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Reaxys Registry Number
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Reaxys
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24533295
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PubMed citation
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Europe PMC
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7902657
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PubMed citation
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Europe PMC
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