DC Chemicals · Product datasheet

AG-1478 (Tyrphostin AG-1478) — Datasheet

CAT. NO. DC1078

Product page and current package options

ParameterValue
Chemical NameN-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine
CAS No.153436-53-4
Synonyms4-Quinazolinamine,N-(3-chlorophenyl)-6,7-dimethoxy-;Tyrphostin AG 1478;AG 1478 HYDROCHLORIDE;AG1478;AG-1478;AG-1478 (Tyrphostin AG-1478);N-(3-chlorophenyl)-6,7-dimethoxy-4-Quinazolinamine;N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine;Tyrphostin AG 1478 (AG 1478,NSC-693255);AG-1478 hydrochloride;NSC693255;Tyrphostin;Tyrphostin AG-1478;(3-Chlorophenyl)(6,7-dimethoxyquinazolin-4-yl)amine;AG1478HCl;AG-1478 (NSC-693255);4-(3-CHLOROANILINO)-6,7-DIMETHOXYQUINAZOLINE HCL;NSC 693255;Tyrphostin AG 1478, free base >99%;AG-1478, 97.5%, a selective EGFR inhibitor;4-(3-Chloroanilino)-6,7-dimethoxyquinazoline;AG 1478;4-Quinazolinamine, N-(3-chlorophenyl)-6,7-dimethoxy-;SUH0SEZ9HY;N-(3-chlorophenyl)-6,7-dimethoxy-quinazolin-4-amine;BRD6408;4-(3-Chloroanilino)-6,7-Dimethoxyquinazoline Hydrochloride
FormulaC16H14ClN3O2
M.Wt315.7543
SMILESClC1=C([H])C([H])=C([H])C(=C1[H])N([H])C1C2=C([H])C(=C(C([H])=C2N=C([H])N=1)OC([H])([H])[H])OC([H])([H])[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

AG-1478 is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM.

In Vitro

AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[3].

In Vivo

AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[3].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Cart

Request quotation