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Tyrphostin AG 1478 (CAS 175178-82-2)

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Alternate Names:
N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinamine
Application:
Tyrphostin AG 1478 is a potent and selective inhibitor of EGFR
CAS Number:
175178-82-2
Purity:
≥98%
Molecular Weight:
315.76
Molecular Formula:
C16H14ClN3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Tyrphostin AG 1478 is a tyrosine kinase inhibitor that has been demonstrated to be a selective and potent inhibitor of EGFR (Epidermal Growth Factor Receptor) in a variety of cell lines with an IC50 of about 3 nM. In Rat-1 fibroblasts, Tyrphostin AG 1478 was demonstrated to downregulate EGF-stimulated DNA synthesis. The induction of p21/cip1/WAF1 and activation of EGF-dependent src-family kinase was noted to be blocked by Tyrphostin AG 1478 in the epidermoid carcinoma cell line A431. Additionally, a study utilizing early-weaned rats to study EGFR signaling and its role in mucosal cell proliferation, the administration of Tyrphostin AG 1478 was noted to decrease ERK phosphorylation without affecting p-Src and p-Akt. Tyrphostin AG 1478 was also noted to reduce measures of mitosis and DNA synthesis in this study. As EGFR is found to be overexpressed in various cancer cells, there may be research interest in compounds that inhibit EGFR, such as Tyrphostin AG 1478.


Tyrphostin AG 1478 (CAS 175178-82-2) References

  1. Niflumic acid and AG-1478 reduce cigarette smoke-induced mucin synthesis: the role of hCLCA1.  |  Hegab, AE., et al. 2007. Chest. 131: 1149-56. PMID: 17426222
  2. Cross-talk between bradykinin and epidermal growth factor in regulating IL-6 production in human airway smooth muscle cells.  |  Feng, PH., et al. 2010. Chang Gung Med J. 33: 92-9. PMID: 20184800
  3. TGF-β1 promotes cell barrier function upon maturation of corneal endothelial cells.  |  Beaulieu Leclerc, V., et al. 2018. Sci Rep. 8: 4438. PMID: 29535350
  4. Role of EGFL7/EGFR-signaling pathway in migration and invasion of growth hormone-producing pituitary adenomas.  |  Liu, Q., et al. 2018. Sci China Life Sci. 61: 893-901. PMID: 29951953
  5. Epidermal-growth-factor-dependent activation of the src-family kinases.  |  Osherov, N. and Levitzki, A. 1994. Eur J Biochem. 225: 1047-53. PMID: 7525285
  6. Prolonged induction of p21Cip1/WAF1/CDK2/PCNA complex by epidermal growth factor receptor activation mediates ligand-induced A431 cell growth inhibition.  |  Fan, Z., et al. 1995. J Cell Biol. 131: 235-42. PMID: 7559780
  7. Tyrosine kinase inhibition: an approach to drug development.  |  Levitzki, A. and Gazit, A. 1995. Science. 267: 1782-8. PMID: 7892601
  8. Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors.  |  Daub, H., et al. 1996. Nature. 379: 557-60. PMID: 8596637
  9. Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors.  |  Han, Y., et al. 1996. Cancer Res. 56: 3859-61. PMID: 8752145
  10. Oxidative stress increases gene expression of heparin-binding EGF-like growth factor and amphiregulin in cultured rat gastric epithelial cells.  |  Miyazaki, Y., et al. 1996. Biochem Biophys Res Commun. 226: 542-6. PMID: 8806670
  11. Opposing effects of tyrosine kinase inhibitors on mineralization of normal and tumor bone cells.  |  Klein, BY., et al. 1997. J Cell Biochem. 65: 420-9. PMID: 9138097
  12. Mapping the binding site for matrix metalloproteinase on the N-terminal domain of the tissue inhibitor of metalloproteinases-2 by NMR chemical shift perturbation.  |  Williamson, RA., et al. 1997. Biochemistry. 36: 13882-9. PMID: 9374866
  13. Opposing effects of cyclosporin A and tyrphostin AG-1478 indicate a role for Src protein in the cellular control of mineralization.  |  Stekelenburg, J., et al. 1998. J Cell Biochem. 71: 116-26. PMID: 9736460

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Tyrphostin AG 1478, 5 mg

sc-200613
5 mg
$94.00

Tyrphostin AG 1478, 25 mg

sc-200613A
25 mg
$413.00