Samiksha Jaiswal (Editor)

AEE788

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CAS Number
  
497839-62-0

IUPHAR/BPS
  
7643

ChEMBL
  
CHEMBL587723

Molar mass
  
440.5832 g/mol

PubChem CID
  
10297043

ChemSpider
  
8472511

Formula
  
C27H32N6

AEE788 httpsuploadwikimediaorgwikipediacommonsthu

Molekyldynamikk aee788


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.

References

AEE788 Wikipedia