Tyrphostin Ag 1478

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CAS: 175178-82-2

Name:

Tyrphostin Ag 1478

Other names:

Tyrphostin AG-1478; AG 1478; N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine; AG-1478 hydrochloride; AG-1478; AG1478

Tyrphostin AG 1478 is a tyrosine kinase inhibitor that has been demonstrated to be a selecetive and potent inhibitor of EGFR (Epidermal Growth Factor Receptor ) in a variety of cell lines with an IC50 of about 3 nM. In Rat-1 fibroblasts, Tyrphostin AG 1478 was demonstrated to downregulate EGF-stimulated DNA synthesis. The induction of p21/ip1/WAF1 and activation of EGF-dependent src-family kinase was noted to be blocked by Tyrphostin AG 1478 in the epidermoid carcinoma cell line A431. Additionally, a study utilizing early-weaned rats to study EGFR signaling and its role in mucosal cell proliferation, the administration of Tyrphostin AG 1478 was noted to decrease ERK phosphorylation without affecting p-Src and p-Akt. Tyrphostin AG 1478 was also noted to reduce measures of mitosis and DNA synthesis in this study. As EGFR is found to be overexpressed in various cancer cells, there may be research interest in compounds that inhibit EGFR, such as Tyrphostin AG 1478.

Interactions

Description

UniProt ID

Protein: C-type lectin domain family 14 member A, Gene: CLEC14A
Protein: Proto-oncogene tyrosine-protein kinase Src, Gene: SRC
Protein: Equilibrative nucleoside transporter 1, Gene: SLC29A1
Protein: Fructose-1,6-bisphosphatase 1, Gene: FBP1
Protein: Fructose-1,6-bisphosphatase isozyme 2, Gene: FBP2
Protein: Tyrosine-protein kinase Lck, Gene: LCK
Protein: Mitogen-activated protein kinase 14, Gene: MAPK14

Toxicity

oral LD50 [mouse] mg/kg
Unavailable
oral LD50 [rat] mg/kg
Unavailable
oral LD50 [rabbit] mg/kg
Unavailable

Effects on organism

Anti Cancer
Antibacterial

No

Antifungal

No

Antiviral

No

Longevity mechanisms activation

No data

Suppression of aging mechanisms

No data

Relation to biomarkers of Aging

Data not available

Relation to aging associated genes

No data available

Experimental conditions

Not available

Life Extension

Mean LS (%)
19.5
Median LS (%)
Mortality rate derease (%)
Max LS (%)
Cell CLS
Cell RLS

Concentration wth maximum effect

100 mkM

More info about experiment

22363408 24134630
Opposite effectNo