Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Cell permeable: yes

Primary TargetEGFR

Target K_i: 6 pM against epidermal growth factor receptor (EGFR)

General description

An extremely potent, cell-permeamble, reversible, ATP-competitive and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀ = 25 pM; K_i = 6 pM). Rapidly suppresses autophosphorylation of EGFR at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells. Also selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. A 10 mM (500 µg/139 µl) solution of PD 153035 (Cat. No. 234491) in DMSO is also available.

An extremely potent, cell-permeamble, reversible, ATP-competitive and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀ = 25 pM; K_i = 6 pM). Rapidly suppresses autophosphorylation of EGFR at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells. Also selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression and oncogenic transformation.

Legal Information

Sold under license of U.S. Patent 5,457,105 and European Patent 0,566,266.

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

Other Notes

Bridges, A.J., et al. 1996. J. Med. Chem. 39, 267.Fry, D.W., et al. 1994. Science265, 1093.

Packaging

1 mg 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)