Drug intelligence / Profile preview

tyrphostin AG1478

Development stage
Preclinical
Lead developer
Hebrew University of Jerusalem
Modality
Small Molecules
Administration
Intraperitoneal, Intratumoral, Intravenous, Intravitreal
01

Overview

Tyrphostin AG1478 (also known as AG1478) is a potent, selective, and reversible small-molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 3 nM. Developed as part of the tyrphostin class of tyrosine kinase inhibitors, it competitively binds to the ATP-binding site of the EGFR kinase domain. Beyond its primary target, AG1478 has been shown to inhibit phosphatidylinositol 4-kinase alpha (PI4KA) and the Golgi-specific brefeldin A-resistance guanine nucleotide exchange factor 1 (GBF1), which contributes to its broad-spectrum antiviral activity against viruses such as encephalomyocarditis virus (EMCV), hepatitis C virus (HCV), and influenza A. It is widely utilized as a research reagent to study EGFR-mediated signaling pathways, cell proliferation, migration, and tissue remodeling in various preclinical models of cancer, asthma, and polycystic kidney disease.

Other names
4-(3-chloroanilino)-6,7-dimethoxyquinazolineN-(3-chlorophenyl)-6,7-dimethoxy-4-quinazolinamineN-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)KCNA5 (Ultra-rapid delayed rectifier potassium channel)GBF1 (Brefeldin A-resistance guanine nucleotide exchange factor 1)PI4KA (PI4Kα)

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