170449-18-0
170449-18-0 structure
- Name: AG 1478 hydrochloride
- Chemical Name: N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride
- CAS Number: 170449-18-0
- Molecular Formula: C16H15Cl2N3O2
- Molecular Weight: 352.215
- Catalog: Signaling Pathways Anti-infection HCV
- Create Date: 2018-11-28 18:42:36
- Modify Date: 2024-01-02 09:57:33
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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].
| Name | N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride |
|---|---|
| Synonyms |
N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinamine hydrochloride (1:1)
6,7-Dimethoxy-4-[N-(3-chlorophenyl)amino]quinazoline hydrochloride N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride (1:1) 4-Quinazolinamine, N-(3-chlorophenyl)-6,7-dimethoxy-, hydrochloride (1:1) N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine,hydrochloride 6,7-Dimethoxy-4-[N-(3-chlorophenyl)amino]quinazolinehydrochloride |
| Description | 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]. |
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| Related Catalog | |
| Target |
EGFR:3 nM (IC50) HCV EMCV |
| 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 | 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]. |
| References |
| Density | 1.337g/cm3 |
|---|---|
| Boiling Point | 458.5ºC at 760mmHg |
| Molecular Formula | C16H15Cl2N3O2 |
| Molecular Weight | 352.215 |
| Flash Point | 231.1ºC |
| Exact Mass | 351.054138 |
| PSA | 56.27000 |
| LogP | 4.91900 |
| Vapour Pressure | 1.37E-08mmHg at 25°C |
| HS Code | 2933990090 |
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| HS Code | 2933990090 |
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| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |