Biochem/physiol Actions
Reversible: no
Product does not compete with ATP.
Target IC50: 250-490 pM inhibiting EGF-receptor (EGFR) kinase activity in vivo; 5 nM inhibiting EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo
Cell permeable: yes
Primary TargetEGFR kinase activity
General description
A cell-permeable and irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM) as well as EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo (IC50 = 5 nM). Blocks EGF-mediated growth in A431 cells. Inhibits proliferation of EGFR or c-ErbB2 expressing cells (IC50 = 31-125 nM) by covalently binding to the EGFR.
A cell-permeable and irreversible inhibitor of EGF-stimulated autophosphorylation of tyrosine residues in the epidermal growth factor receptor (EGFR) in vivo (IC50 = 250-490 pM) and blocks EGF-mediated growth. Also inhibits proliferation of cells that overexpress EGFR or c-Erb-2 (IC50 = 31-125 nM) by covalently binding to EGFR.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Sweeney, W.E., et al. 2000. Kidney Int.57, 33.Discafani, C.M., et al. 1999. Biochem. Pharmacol. 57, 917.Sweeney, W.E., et. al. 1999. Kidney Int.56, 406.
Packaging
1 mg in Plastic ampoule
Packaged under inert gas
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Warning
Toxicity: Standard Handling (A)
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