513035
PD 158780
A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC50 = 8 pM).
别名:
PD 158780, 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine
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关于此项目
经验公式（希尔记法）:
C14H12BrN5
化学文摘社编号:
分子量:
330.18
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
Brc1cc(ccc1)Nc2ncnc3c2cc(nc3)NC
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
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
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General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EGFR tyrosine kinase
EGFR tyrosine kinase
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
Preparation Note
Following reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -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
11 - Combustible Solids
wgk
WGK 3
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