AG-1478

• CAT Number: I001925
• CAS Number: 153436-53-4
• Molecular Formula: C16H14ClN3O2
• Molecular Weight: 315.75
• Purity: ≥95%
• Synonyms: N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine
• Target: EGFR
• Solubility: DMSO 25 mg/mL; Water <1 mg/mL; Ethanol 13 mg/mL
• Storage: 2-8°C
• IC50: 3 nM
• InChI: 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)
• InChIKey: GFNNBHLJANVSQV-UHFFFAOYSA-N
• SMILES: COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Cl)OC

AG-1478 (Cat No.:I001925) is a highly selective inhibitor of the epidermal growth factor receptor (EGFR). With an IC50 value of 3 nM, it effectively inhibits EGFR activity. Notably, AG-1478 displays minimal activity against other receptor tyrosine kinases such as HER2-Neu, PDGFR, Trk, Bcr-Abl, and InsR. This selectivity makes AG-1478 a valuable tool in studying EGFR signaling pathways and exploring its potential as a therapeutic agent for EGFR-dependent cancers while minimizing off-target effects on other receptor systems.

Reference

1:UV-Vis spectroscopy and solvatochromism of the tyrosine kinase inhibitor AG-1478. Khattab M, Wang F, Clayton AH.Spectrochim Acta A Mol Biomol Spectrosc. 2016 Jul 5;164:128-32. doi: 10.1016/j.saa.2016.04.009. Epub 2016 Apr 12. PMID: 27092736 2:The EGFR tyrosine kinase inhibitor tyrphostin AG-1478 causes hypomagnesemia and cardiac dysfunction. Weglicki WB, Kramer JH, Spurney CF, Chmielinska JJ, Mak IT.Can J Physiol Pharmacol. 2012 Aug;90(8):1145-9. doi: 10.1139/y2012-023. Epub 2012 May 30. PMID: 22646904 Free PMC Article3:Niflumic acid and AG-1478 reduce cigarette smoke-induced mucin synthesis: the role of hCLCA1. Hegab AE, Sakamoto T, Nomura A, Ishii Y, Morishima Y, Iizuka T, Kiwamoto T, Matsuno Y, Homma S, Sekizawa K.Chest. 2007 Apr;131(4):1149-56. PMID: 17426222 4:Fluorescence and analytical ultracentrifugation analyses of the interaction of the tyrosine kinase inhibitor, tyrphostin AG 1478-mesylate, with albumin. Clayton AH, Perugini MA, Weinstock J, Rothacker J, Watson KG, Burgess AW, Nice EC.Anal Biochem. 2005 Jul 15;342(2):292-9. PMID: 15913535 5:Direct inhibition of the cloned Kv1.5 channel by AG-1478, a tyrosine kinase inhibitor. Choi BH, Choi JS, Rhie DJ, Yoon SH, Min DS, Jo YH, Kim MS, Hahn SJ.Am J Physiol Cell Physiol. 2002 Jun;282(6):C1461-8. PMID: 11997261 Free Article6:Opposing effects of cyclosporin A and tyrphostin AG-1478 indicate a role for Src protein in the cellular control of mineralization. Stekelenburg J, Klein BY, Ben-Bassat H, Rojansky N.J Cell Biochem. 1998 Oct 1;71(1):116-26. PMID: 9736460 7:Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors. Han Y, Caday CG, Nanda A, Cavenee WK, Huang HJ.Cancer Res. 1996 Sep 1;56(17):3859-61. PMID: 8752145 Free Article