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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
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

Key Documents

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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

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
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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

513035-1.1ML: + 513035-VUG: + 513035-500UG:

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Certificates of Analysis (COA)

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Global Trade Item Number

SKUGTIN
513035-500UGCN04055977198645

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