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ChEBI

PD158780

Term ID
CHEBI:92843
Synonyms
  • 4-(3-bromoanilino)-6-(methylamino)pyrido[3,4-d]pyrimidine
  • 4-(3-bromoanilino)-6-methylaminopyrido[3,4-d]pyrimidine
  • 4-[(3-bromophenyl)amino]-6-(methylamino)pyrido[3,4-d]pyrimidine
  • N(4)-(3-bromophenyl)-N(6)-methylpyrido[3,4-d]pyrimidine-4,6-diamine
  • PD 158780
  • PD-158780
Definition
A pyridopyrimidine that is pyrido[3,4-d]pyrimidine-4,6-diamine in which the amino groups at positions 4 and 6 are substituted by a m-bromophenyl group and a methyl group, respectively. It is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity [IC50 values of 0.008, 49 and 52 nM for EGFR, ErbB2 (HER2) and Erb4 (HER4)]. It does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells.
References
  • cas:171179-06-9
  • lincs.smallmolecule:LSM-3069
  • pubmed:10368634
  • pubmed:12548551
  • pubmed:15572027
  • pubmed:17079657
  • pubmed:22354538
  • pubmed:27988307
  • pubmed:9354588
  • pubmed:9513602
  • pubmed:9603960
  • reaxys:7487408
Ontology
ChEBI  ( EBI )
Relationships
Phenotype
Phenotype resulting from PD158780
Phenotype where environments contain PD158780
Phenotype modified by environments containing PD158780
Phenotype affecting PD158780
Human Disease Model