| Identification | Back Directory | [Name]
TYRPHOSTIN AG 1296 | [CAS]
146535-11-7 | [Synonyms]
1296
AG 1296
AG-1296;AG 1296;
TYRPHOSTIN AG 1296
TYRPHOSTIN AG 1296 USP/EP/BP
Tyrphostin AG 1296 (AG 1296)
AG-1296
(Tyrphostin AG 1296)
6,7-DIMETHOXY-2-PHENYLQUINOXALINE
6,7-DIMETHOXY-3-PHENYLQUINOXALINE
Quinoxaline,6,7-dimethoxy-2-phenyl-
AG 1296 - CAS 146535-11-7 - Calbiochem | [Molecular Formula]
C16H14N2O2 | [MDL Number]
MFCD00270913 | [MOL File]
146535-11-7.mol | [Molecular Weight]
266.29 |
| Chemical Properties | Back Directory | [Boiling point ]
420.2±40.0 °C(Predicted) | [density ]
1.192±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°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. |
| Hazard Information | Back Directory | [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.1 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).2 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. 2 Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype.2 | [Uses]
A potent inhibitor of PDGF receptor tyrosine kinase (IC50=1 μM). Also inhibits FGF receptor tyrosine kinase and c-kit. Induces apoptosis in a small-cell lung cancer cell line (H526). | [Definition]
ChEBI: 6,7-dimethoxy-2-phenylquinoxaline is a quinoxaline derivative. | [in vivo]
Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo[4].
?
Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype[5]. | Animal Model: | Nud/nud mice are injected with A375R cells[4] | | Dosage: | 40, 80 mg/kg | | Administration: | I.p. daily for two weeks | | Result: | Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.
Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.
|
| [target]
PDGFR | [IC 50]
PDGFRα; PDGFRβ | [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 |
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| Company Name: |
Spectrum Chemical Manufacturing Corp.
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| Tel: |
021-021-021-67601398-809-809-809 15221380277 |
| Website: |
www.spectrumchemical.com/oa_html/index.jsp?minisite=10020&respid=22372&language=us |
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