PD 158780A potent tyrosine kinase inhibitor that can permeate cells

PD 158780 (CAS 171179-06-9)

  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getAggregateRating, 74ms
  • REVIEWS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;
Synonym: 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine; N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
Application: A potent tyrosine kinase inhibitor that can permeate cells
CAS Number: 171179-06-9
Purity: ≥99%
Molecular Weight: 330.18
Molecular Formula: C14H12BrN5
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

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.


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

Appearance :
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 :
~1.6 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

Adobe Acrobat Reader is required to reliably view,
print and comment on PDF documents

  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getContent, 166ms
  • QUESTIONS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getReviews, 3ms
  • REVIEWS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;

Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2019 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.