| Identification | Back Directory | [Name]
6,7-Dimethoxy-4-[N-(3-chlorophenyl)amino]quinazoline hydrochloride | [CAS]
170449-18-0 | [Synonyms]
-6,7-dimethoxyquinazolin-4-amine hydrochloride
N-(3-chlorophenyl)-6,7-dimethoxy- hydrochloride
N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine HCl
N-(3-chlorophenyl)-6,7-diMethoxyquinazolin-4-aMine hydrochloride
N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinamine hydrochloride
6,7-Dimethoxy-4-[N-(3-chlorophenyl)amino]quinazoline hydrochloride | [Molecular Formula]
C16H14ClN3O2.HCl | [MDL Number]
MFCD06804597 | [MOL File]
170449-18-0.mol |
| Hazard Information | Back Directory | [Uses]
AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV)[1][2][3][4]. | [Definition]
ChEBI: A member of the class of quinazolines that is quinazoline substituted by methoxy groups at positions 6 and 7 and a (3-chlorophenyl)nitrilo group at position 4. It acts as an epidermal growth factor receptor antagonist. | [in vivo]
Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE-/- mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG)[2]. Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478[3]. | [IC 50]
EGFR: 3 nM (IC50); HCV; EMCV | [storage]
Desiccate at -20°C | [References]
[1] Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95. DOI:10.5603/fhc.2012.0028
[2] Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580. DOI:10.1038/srep24580
[3] Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215. DOI:10.1371/journal.pone.0132215
[4] Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6. DOI:10.1128/AAC.01331-16 |
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