ag-1478-tyrphostin-ag-1478

Description: AG-1478 (also known as Tyrphostin AG1478; AG-1478; NSC-693255) is a novel, potent and selective EGFR (epidermal growth factor receptor) inhibitor with potential antitumor and antidiabetic activity. It inhibits EGFR with an IC50 of 3 nM in cell-free assays. AG-1478 also 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 shows potent anti-proliferative activity in vitro against 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)

Chemical Name: N-(3-chlorophenyl)-6, 7-dimethoxyquinazolin-4-amine

InChi Key: GFNNBHLJANVSQV-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H14ClN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H, 1-2H3, (H, 18, 19, 20)

SMILES Code: COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC