513036
PD 158780
InSolution, ≥95%, EGFR tyrosine kinase activity inhibitor
别名:
InSolution PD 158780
InChI
1S/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20)
InChI key
KFHMLBXBRCITHF-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
shipped in
wet ice
storage temp.
−20°C
Quality Level
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General description
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
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
Physical form
A 10 mM (500 µg/151 µl) solution of PD 158780 (Cat. No. 513035) in DMSO.
Preparation Note
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.
Rewcastle, G.W., et al. 1998. J. Med. Chem.41, 742.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
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