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

Ontology

ChEBI ( EBI )

Relationships

is a type of: aromatic amine bromobenzenes diamine pyridopyrimidine secondary amino compound

aromatic amine bromobenzenes diamine pyridopyrimidine secondary amino compound Show first 5 Terms
has_role: antineoplastic agent EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor

antineoplastic agent EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor Show first 5 Terms

Phenotype

Phenotype resulting from PD158780

Phenotype where environments contain PD158780

Phenotype modified by environments containing PD158780

Human Disease Model