AG1478 HCl (Tyrphostin AG-1478)

Description: AG-1478 HCl (also known as Tyrphostin AG-1478) is a novel, potent and selective EGFR (epidermal growth factor receptor) inhibitor with IC50 of 3 nM in cell-free assays. It reversibly inhibits rat brain Kv1.5 potassium channels with IC50 of 9.8 uM which is independent of protein tyrosine kinase (PTK) activity. AG-1478 also inhibits the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 uM, respectively. Previous studies suggest that EGFR antagonism may be effective for the treatment of various diseases such as cancer, angiotensin II-induced cardiac hypertrophy and diabetic cardiomyopathy. Therefore, AG-1478 has the potential to be used as therapeutics for these disorders.

References: Cancer Res. 1996; 56(17):3859-61; Proc Natl Acad Sci U S A. 2003; 100(26):15871-6.

Related CAS #: 170449-18-0 (HCl); 153436-53-4 (free)