Molecular structure of PD 158780, CAS Number: 171179-06-9
PD 158780 (CAS 171179-06-9)
See product citations (2)
Alternate Names:
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:
PD 158780 is a potent tyrosine kinase inhibitor that can permeate cells
CAS Number:
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.
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SDS & Certificate of Analysis
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.
PD 158780 (CAS 171179-06-9) References
- Growth inhibition of nasopharyngeal carcinoma cells by EGF receptor tyrosine kinase inhibitors. | Sun, Y., et al. 1999. Anticancer Res. 19: 919-24. PMID: 10368634
- Epidermal growth factor receptor tyrosine kinase inhibitors as anticancer agents. | Ciardiello, F. 2000. Drugs. 60 Suppl 1: 25-32; discussion 41-2. PMID: 11129169
- Why the epidermal growth factor receptor? The rationale for cancer therapy. | Baselga, J. 2002. Oncologist. 7 Suppl 4: 2-8. PMID: 12202782
- Dissociation of focal adhesion kinase and paxillin tyrosine phosphorylation induced by bombesin and lysophosphatidic acid from epidermal growth factor receptor transactivation in Swiss 3T3 cells. | Salazar, EP., et al. 2003. J Cell Physiol. 194: 314-24. PMID: 12548551
- E-cadherin binding modulates EGF receptor activation. | Fedor-Chaiken, M., et al. 2003. Cell Commun Adhes. 10: 105-18. PMID: 14681060
- G1 cell cycle arrest due to the inhibition of erbB family receptor tyrosine kinases does not require the retinoblastoma protein. | Gonzales, AJ. and Fry, DW. 2005. Exp Cell Res. 303: 56-67. PMID: 15572027
- [Small-molecule tyrosine kinase inhibitors of epidermal growth factor receptor (EGFR)]. | Mitsudomi, T. 2009. Gan To Kagaku Ryoho. 36: 1058-62. PMID: 19620791
- Interleukin-6 and neuregulin-1 as regulators of utrophin expression via the activation of NRG-1/ErbB signaling pathway in mdx cells. | Juretić, N., et al. 2017. Biochim Biophys Acta Mol Basis Dis. 1863: 770-780. PMID: 27988307
- Zonisamide upregulates neuregulin-1 expression and enhances acetylcholine receptor clustering at the in vitro neuromuscular junction. | Inoue, T., et al. 2021. Neuropharmacology. 195: 108637. PMID: 34097946
- Recombinant human neuregulin-1 alleviates immobilization-induced neuromuscular dysfunction via neuregulin-1/ErbB signaling pathway in rat. | Yang, J., et al. 2023. Arch Biochem Biophys. 743: 109631. PMID: 37276924
- Biochemical and antiproliferative properties of 4-[ar(alk)ylamino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. | Fry, DW., et al. 1997. Biochem Pharmacol. 54: 877-87. PMID: 9354588
- Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors. | Rewcastle, GW., et al. 1998. J Med Chem. 41: 742-51. PMID: 9513602
- Role of tyrosine kinase activity of epidermal growth factor receptor in the lysophosphatidic acid-stimulated mitogen-activated protein kinase pathway. | Cunnick, JM., et al. 1998. J Biol Chem. 273: 14468-75. PMID: 9603960
Inhibitor of:
EGFR, ErbB-4, Neu, and Tyrosine Kinase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PD 158780, 10 mg | sc-358789 | 10 mg | $127.00 |