AG 1478

AG-1478 (175478-82-2; base) is a potent and selective inhibitor of the EGFR kinase (IC50 = 3 nM). Inhibits proliferation of a variety human cancer cell lines.1,2 AG-1478 reduces pulmonary fibrosis in a rat model.3?Cell permeable.

Tyrphostin AG 1478 is a potent and selective inhibitor of EGFR.

Tyrphostin AG 1478 has been used as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor to study its effect on desmoid cell mobility in boyden chamber motility assays. It has also been used to inhibit phosphorylation of c-Met by exogenous transforming growth factor α in epidermoid carcinoma cell line A431.

A highly potent and specific EGFR tyrosine kinase inhibitor with an IC50 of 3 nM.

ChEBI: Tyrphostin AG 1478 is a member of the class of quinazolines that is quinazoline substituted by methoxy groups at positions 6 and 7 and a (3-chlorophenyl)nitrilo group at position 4. It acts as an epidermal growth factor receptor antagonist. It has a role as an epidermal growth factor receptor antagonist, an antineoplastic agent, a geroprotector and an antiviral agent. It is a member of quinazolines, an aromatic ether and a member of monochlorobenzenes.

Highly potent and specific inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (IC₅₀ = 3 nM). Much higher concentrations are required for inhibition of the kinase activity of the closely related HER2 (neu/erb-B2) receptor (IC₅₀ >100 μM), the platelet-derived growth factor (PDGF) receptor (IC₅₀ >100 μM), and p210^Bcr-Abl (IC₅₀ >50 μM). Its mechanism of inhibition likely mimics that of the related compound, 4-(3-chloroanilino)quinazoline (CAQ), a competitive inhibitor with respect to ATP.

Primary TargetEpidermal growth factor receptor kinase

[1] Y HAN. Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors.[J]. Cancer research, 1996, 56 17: 3859-3861.
[2] G PARTIK. Inhibition of epidermal-growth-factor-receptor-dependent signalling by tyrphostins A25 and AG1478 blocks growth and induces apoptosis in colorectal tumor cells in vitro.[J]. Journal of Cancer Research and Clinical Oncology, 1999, 125 7: 379-388. DOI:10.1007/s004320050290
[3] ANNETTE B. RICE . Specific Inhibitors of Platelet-Derived Growth Factor or Epidermal Growth Factor Receptor Tyrosine Kinase Reduce Pulmonary Fibrosis in Rats[J]. American Journal of Pathology, 1999, 155 1: Pages 213-221. DOI:10.1016/s0002-9440(10)65115-2