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Merck

513035

PD 158780

A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC50 = 8 pM).

Synonym(s):

PD 158780, 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine

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About This Item

Empirical Formula (Hill Notation):
C14H12BrN5
CAS Number:
171179-06-9
Molecular Weight:
330.18
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00942160

Key Documents

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Product Name

PD 158780, A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC50 = 8 pM).

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

100

Related Categories

Biochem/physiol Actions

Cell permeable: yes
Primary Target
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

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

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

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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Global Trade Item Number

SKUGTIN
513035-500UGCN04055977198645

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