| Identification | Back Directory | [Name]
PD158780 | [CAS]
171179-06-9 | [Synonyms]
PD 158780 solution
PD 158780; PD-158780
InSolution? PD 158780
PD 158780 - CAS 171179-06-9 - Calbiochem
InSolution PD 158780 - CAS 171179-06-9 - Calbiochem
N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl-
Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl- (Related Reference) | [Molecular Formula]
C14H12BrN5 | [MDL Number]
MFCD00942160 | [MOL File]
171179-06-9.mol | [Molecular Weight]
330.188 |
| Chemical Properties | Back Directory | [Melting point ]
174.0 to 178.0 °C | [Boiling point ]
499.6±45.0 °C(Predicted) | [density ]
1.611±0.06 g/cm3 (20 ºC 760 Torr) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: ≥20mg/mL | [form ]
Yellow solid | [pka]
5.80±0.30(Predicted) | [color ]
yellow |
| Hazard Information | Back Directory | [Uses]
PD 158780 is a potent tyrosine kinase inhibitor of the epidermal growth factor receptor and has been shown to delay substantial growth of tumors in vivo tumor models. | [Definition]
ChEBI: PD158780 is 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. It has a role as an antineoplastic agent and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a pyridopyrimidine, a secondary amino compound, a member of bromobenzenes, a diamine and an aromatic amine. | [General Description]
A potent inhibitor of the EGFR tyrosine kinase activity (8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC50 =49 nM) and MDA-MB-453 (IC50 = 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells. | [Biological Activity]
Potent inhibitor of ErbB receptor family tyrosine kinases (IC 50 values are 0.008, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively) that does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G 1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells. | [Biochem/physiol Actions]
Cell permeable: yes | [storage]
Store at -20°C |
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