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513035 Sigma-Aldrich

PD 158780 - CAS 171179-06-9 - Calbiochem

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

Synonym: 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine, PD 158780 - CAS 171179-06-9 - Calbiochem

  • CAS Number 171179-06-9

  • Empirical Formula (Hill Notation) C14H12BrN5

  • Molecular Weight 330.18

  •  MDL number MFCD00942160

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Properties

Related Categories Biochemicals and Reagents, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, P to Q,
Quality Level   100
assay   ≥95% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
color   yellow
solubility   DMSO: 5 mg/mL
shipped in   ambient

Description

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 ½ (MKK½) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells.

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.

Packaging

500 μg in Plastic ampoule

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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