PD 158780-CAS 171179-06-9-Calbiochem

产品说明

一般描述

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.

包装

500 μg in Plastic ampoule
Packaged under inert gas

生化/生理作用

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
Primary Target
EGFR tyrosine kinase
Product competes with ATP.
Reversible: yes

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

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

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