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Merck

513036

PD 158780

InSolution, ≥95%, EGFR tyrosine kinase activity inhibitor

Synonym(s):

InSolution PD 158780

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About This Item

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

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Product Name

PD 158780, InSolution, ≥95%, EGFR tyrosine kinase activity inhibitor

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

100

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

Disclaimer

Toxicity: Standard Handling (A)

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.

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

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).

Legal Information

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

Storage Class

10 - Combustible liquids

wgk

WGK 2

flash_point_f

188.6 °F - closed cup - (Dimethylsulfoxide)

flash_point_c

87 °C - closed cup - (Dimethylsulfoxide)

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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