513035

PD 158780

A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC₅₀ = 8 pM).

• Sinonimo/i: PD 158780, 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine
• Formula empirica (notazione di Hill): C₁₄H₁₂BrN₅
• Numero CAS: 171179-06-9
• Peso molecolare: 330.18
• Numero MDL: MFCD00942160
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: yellow
• Solubilità: DMSO: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C
• InChI: 1S/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20); KFHMLBXBRCITHF-UHFFFAOYSA-N

Descrizione

Descrizione generale

A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC₅₀ = 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 ½ (MKK½) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells.

A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC₅₀ = 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 NIH 3T3 cells. A 10 mM (500 µg/151 µl) solution of PD 158780 (Cat. No. 513036) in DMSO is also available.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
EGFR tyrosine kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 8 pM against EGFR tyrosine kinase activity; 49 nM, 52 nm, against heregulin-stimulated autophosphorylation in SK-BR-3 and MDA-MB-453 breast carcinomas, respectively

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.

Altre note

Cunnick, J.M., et al. 1998. J. Biol. Chem. 273, 14468.
Rewcastle, G.W., et al. 1998. J. Med. Chem.41, 742.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3