PD 158780 CAS: 171179-06-9
MF: C14H12BrN5
MW: 330.18
A potent tyrosine kinase inhibitor that can permeate cells.

PD 158780 (CAS 171179-06-9)

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Alternativa namn: 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine; N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
Ansökan PD 158780 is a potent tyrosine kinase inhibitor that can permeate cells
Momsregistreringsnummer :: 171179-06-9
Purity: ≥99%
Molecular Weight: 330.18
Molecular Formula: C14H12BrN5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

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.


Konferenser

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

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (25 mM).
LAGRING :
Store at -20° C
Melting Point :
186.23° C (Predicted)
Boiling Point :
~499.56° C at 760 mmHg (Predicted)
Density :
~1.6 g/cm3 (Predicted)
Refractive Index :
n20D 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)
pK Values :
pKb: 5.80 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
4707
MDL Number :
MFCD00942160
SMILES :
CNC1=NC=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br

Download SDS (MSDS)

Certificate of Analysis

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