PD 158780 (CAS 171179-06-9)

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Synonym:	4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine
Application:	A potent tyrosine kinase inhibitor that can permeate cells
CAS Number:	171179-06-9
Purity:	≥99%
Molecular Weight:	330.2
Molecular Formula:	C₁₄H₁₂BrN₅

Description

The compound PD 158780 is a potent tyrosine kinase inhibitor that can permeate cells and shows no inhibition against FGF or PDGF-mediated tyrosine phosphorylation. PD 158780 shows high specificity for inhibiting EGF-dependent autophosphorylation and can inhibit other members of the EGF-receptor family, such as Neuregulin-1 (heregulin)-stimulated phosphorylation. Research shows that PD 158780 can cause G1 cell cycle arrest through the inhibition of erbB family (EGFR, Neu, ErbB-3, and ErbB-4) receptor tyrosine kinase activity in the breast epithelial cell line MCF10A. Studies show that LPA-stimulated MAPK kinase activation and EGFR tyrosine phosphorylation in HeLa and NIH 3T3 cells can be inhibited by PD 158780. It has been observed that PD 158780 has anti-proliferative activity in A431 human epidermal carcinoma cells.

Technical Information

Appearance:	Yellow powder
Physical State:	Solid
Solubility:	Soluble in DMSO (100 mM), and ethanol (25 mM).
Storage:	Store at -20° C
Melting Point:	186.23 °C (Predicted)
Boiling Point:	499.56 °C at 760 mmHg (Predicted)
Density:	1.61 g/cm³ (Predicted)
Refractive Index:	n²⁰_D 1.77 (Predicted)
IC50:	EGFR: IC₅₀ = 0.01 nM; ErbB2: IC₅₀ = 49 nM; ErbB2/ErbB4: IC₅₀ = 52 nM; A-431: IC₅₀ = 13 nM (human); MAP kinase-interacting serine/threonine-protein kinase MNK1 : IC₅₀ = 1700 nM (human)

Safety and Reference Information

SMILES:

CNC1NCC2NCNC(NC3CCCC(Br)C3)C2C1

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

References

1. Fry, D.W., et al. 1997. Biochem. Pharmacol. 54: 877-887. PMID: 9354588
2. Cunnick, J.M., et al. 1998. J. Biol. Chem. 273: 14468-14475. PMID: 9603960
3. Rewcastle, G.W., et al. 1998. J. Med. Chem. 41: 742-751. PMID: 9513602
4. Sun, Y., et al. 1999. Anticancer Res. 19: 919-924. PMID: 10368634
5. Gonzales, A.J., et al. 2005. Exp. Cell Res. 303: 56-67. PMID: 15572027

SDS

Datasheet/SDS