6,7-Dimethoxy-3-phenylquinoxaline
1296 · AG 1296 · A 1296 · AG-1296 · TYRPHOSTIN AG 1296 · Tyrphostin AG 1296 ，S8024 · TYRPHOSTIN AG 1296 USP/EP/BP · Tyrphostin AG 1296 (AG 1296)
Identifikatoren & physikalische Daten
| CAS No. | 146535-11-7 |
|---|---|
| Summenformel | C16H14N2O2 |
| Durchschnittliche Molmasse | 266,29 g/mol |
| Monoisotopische Masse | 266,10552769 g/mol |
| SMILES | COc1cc2ncc(-c3ccccc3)nc2cc1OC |
| InChIKey | QNOXYUNHIGOWNY-UHFFFAOYSA-N |
| PubChem CID | 2049 |
| ChEMBL | CHEMBL71191 |
| ChEBI | CHEBI:93335 |
| DTXSID | DTXSID70163393 |
Chemische & physikalische Eigenschaften
| XLogP | 2,8 |
|---|---|
| Polarare Oberfläche (TPSA) | 44,2 |
| H-Brücken-Donoren | 0 |
| H-Brücken-Akzeptoren | 4 |
| Frei drehbare Bindungen | 3 |
| Schwere Atome | 20 |
| Formalladung | 0 |
| Komplexität | 307 |
| Siedepunkt | 420.2±40.0 °C(Predicted) |
| Dichte | 1.192±0.06 g/cm3(Predicted) |
| Lagerbedingungen | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| Löslichkeit | Soluble in DMSO. |
| pKa (Säurekonstante) | 0.48±0.30(Predicted) |
| Aggregatzustand | White solid |
| Farbe | Yellow |
| Stabilität | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| InChI | 1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3 |
| InChIKey | QNOXYUNHIGOWNY-UHFFFAOYSA-N |
Sicherheit & Vorschriften
| Wassergefährdungsklasse (WGK) | 3 |
|---|---|
| Lagerklasse | 11 - Combustible Solids |
Anwendungen & Verwendung
Beschreibung
Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of atherosclerosis, restenosis, pulmonary fibrosis, and gliomas. AG-1296 is a potent and selective inhibitor of PDGF receptor kinase with an IC50 value of about 0.4 μM both in vitro and in cells (Swiss 3T3 cells). It inhibits ligand-stimulated DNA synthesis in platelet-derived growth factor receptor and stem cell factor/kit receptor transfected cells with an IC50 values of 1.5 and 1.8 μM, respectively. Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.
Verwenden
Tyrphostin AG 1296, is the platelet-derived growth factor receptor (PDGFR) inhibitor, which can causes growth inhibition in glioblastoma cells.