| 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. |
