AG 1478

Bezeichnung:AG 1478

CAS-Nr175178-82-2

Englisch Name:AG 1478

CBNumberCB8751920

SummenformelC16H14ClN3O2

Molgewicht315.75

MOL-Datei175178-82-2.mol

AG 1478 physikalisch-chemischer Eigenschaften

Schmelzpunkt	180 - 183°C
storage temp.	2-8°C
Löslichkeit	0.1 M HCl: soluble <0.4 mg/mL
Aggregatzustand	Pale yellow solid
Farbe	Off-white
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.

Sicherheit

WGK Germany

AG 1478 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
AG-1478 (175478-82-2; base) is a potent and selective inhibitor of the EGFR kinase (IC50 = 3 nM). Inhibits proliferation of a variety human cancer cell lines.1,2 AG-1478 reduces pulmonary fibrosis in a rat model.3?Cell permeable.
Verwenden
A highly potent and specific EGFR tyrosine kinase inhibitor with an IC50 of 3 nM.
Verwenden
Tyrphostin AG 1478 is a potent and selective inhibitor of EGFR.
Verwenden
Tyrphostin AG 1478 has been used as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor to study its effect on desmoid cell mobility in boyden chamber motility assays. It has also been used to inhibit phosphorylation of c-Met by exogenous transforming growth factor α in epidermoid carcinoma cell line A431.
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.
Allgemeine Beschreibung
Highly potent and specific inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (IC₅₀ = 3 nM). Much higher concentrations are required for inhibition of the kinase activity of the closely related HER2 (neu/erb-B2) receptor (IC₅₀ >100 μM), the platelet-derived growth factor (PDGF) receptor (IC₅₀ >100 μM), and p210^Bcr-Abl (IC₅₀ >50 μM). Its mechanism of inhibition likely mimics that of the related compound, 4-(3-chloroanilino)quinazoline (CAQ), a competitive inhibitor with respect to ATP.
Biochem/physiol Actions
Primary TargetEpidermal growth factor receptor kinase
Einzelnachweise
1) Han et al. (1996), Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors; Cancer Res., 56 3859 2) Partik et al. (1999), Inhibition of epidermal-growth-factor-receptor-dependent signaling by tyrphostins A25 and AG1478 blocks growth and induces apoptosis in colorectal tumor cells in vitro; J. Cancer Res. Clin. Oncol., 125 379 3) Rice et al. (1999), Specific inhibitors of platelet-derived growth factor or epidermal growth factor receptor tyrosine kinase reduce pulmonary fibrosis in rats; Am. J. Pathol., 155 213

AG 1478 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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