Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetEGFR tyrosine kinase

Cell permeable: 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

General description

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

500 µg in Plastic ampoule

Reconstitution

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

Warning

Toxicity: Standard Handling (A)