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| | TYRPHOSTIN AG 1296 Basic information |
| Product Name: | TYRPHOSTIN AG 1296 | | Synonyms: | TYRPHOSTIN AG 1296;AG 1296;6,7-DIMETHOXY-2-PHENYLQUINOXALINE;6,7-DIMETHOXY-3-PHENYLQUINOXALINE;Quinoxaline,6,7-dimethoxy-2-phenyl-;AG-1296;AG 1296;;AG 1296 - CAS 146535-11-7 - Calbiochem;AG-1296
(Tyrphostin AG 1296) | | CAS: | 146535-11-7 | | MF: | C16H14N2O2 | | MW: | 266.29 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 146535-11-7.mol |  |
| | TYRPHOSTIN AG 1296 Chemical Properties |
| Boiling point | 420.2±40.0 °C(Predicted) | | density | 1.192±0.06 g/cm3(Predicted) | | storage temp. | Keep in dark place,Sealed in dry,Store in freezer, under -20°C | | solubility | Soluble in DMSO. | | form | White solid | | pka | 0.48±0.30(Predicted) | | color | Yellow | | Sensitive | Light Sensitive | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| | TYRPHOSTIN AG 1296 Usage And Synthesis |
| Description | 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. | | Uses | Tyrphostin AG 1296, is the platelet-derived growth factor receptor (PDGFR) inhibitor, which can causes growth inhibition in glioblastoma cells. | | Definition | ChEBI: 6,7-dimethoxy-2-phenylquinoxaline is a quinoxaline derivative. | | target | PDGFR | | References | 1) Kovalenko et al. (1997), Phosphorylation site-specific inhibition of platelet-derived growth factor beta-receptor autophosphorylation by the receptor blocking tyrphostin AG1296; Biochemistry, 36 6260
2) Krystal et al. (1997), Induction of apoptosis and inhibition of small cell lung cancer growth by the quinoxaline tyrphostins; Cancer Res., 57 220
3) Strutz et al. (2001), TGF-beta 1 induces proliferation in human renal fibroblasts via induction of basic fibroblast growth factor (FGF-2); Kidney Int., 59 579 |
| | TYRPHOSTIN AG 1296 Preparation Products And Raw materials |
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