| Identification | Back Directory | [Name]
AG 1478 HYDROCHLORIDE | [CAS]
153436-53-4 | [Synonyms]
AG-1478
AG1478HCl
NSC 693255
AG 1478 HYDROCHLORIDE
AG-1478 (Tyrphostin AG-1478)
Tyrphostin AG 1478, free base >99%
4-(3-CHLOROANILINO)-6,7-DIMETHOXYQUINAZOLINE HCL
(3-Chlorophenyl)(6,7-dimethoxyquinazolin-4-yl)amine
4-(3-CHLOROANILINO)-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE
N-(3-CHLOROPHENYL)-6,7-DIMETHOXY-4-QUINAZOLINANINE HYDROCHLORIDE | [Molecular Formula]
C16H15Cl2N3O2 | [MDL Number]
MFCD06804597 | [MOL File]
153436-53-4.mol | [Molecular Weight]
352.22 |
| Chemical Properties | Back Directory | [Melting point ]
247 °C(dec.) | [Boiling point ]
458.5±45.0 °C(Predicted) | [density ]
1.337 | [storage temp. ]
Desiccate at-20°C | [solubility ]
insoluble in H2O; ≥15.8 mg/mL in DMSO; ≥2.38 mg/mL in EtOH with gentle warming | [form ]
White to light yellow solid. | [pka]
5.54±0.30(Predicted) | [color ]
Light orange to Yellow to Green | [λmax]
332nm(lit.) |
| Hazard Information | Back Directory | [Usage]
A highly potent and specific EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. | [Biological Activity]
Potent and selective inhibitor of epidermal growth factor receptor kinase (IC 50 values 3 nM for EGFR and > 100 μ M for ErbB2 and PDGFR). Inhibits proliferation of NCI-H2170 NSCLC cells in vitro (IC 50 = 1 μ M). | [Uses]
A highly potent and specific EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. | [Definition]
ChEBI: Tyrphostin AG 1478 is 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. It has a role as an epidermal growth factor receptor antagonist, an antineoplastic agent, a geroprotector and an antiviral agent. It is a member of quinazolines, an aromatic ether and a member of monochlorobenzenes. | [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]. | [target]
EGFR | [IC 50]
EGFR: 3 nM (IC50); HCV; EMCV |
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