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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target EGFR
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
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Physical form
A 10 mM (500 µg/151 µl) solution of PD 158780 (Cat. No. 513035) in DMSO.
Reconstitution
Following initial thaw, aliquot and freeze (-20°C).
Other Notes
Cunnick, J.M., et al. 1998. J. Biol. Chem. 273, 14468. Rewcastle, G.W., et al. 1998. J. Med. Chem.41, 742.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
10 - Combustible liquids
wgk_germany
WGK 2
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
Certificates of Analysis (COA)
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