PD 158780 solution (CAS 171179-06-9)
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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 solution (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
- 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
- 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
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PD 158780 solution, 500 µg | sc-202758 | 500 µg | $159.00 |