| Identification | Back Directory | [Name]
AG 1295 | [CAS]
71897-07-9 | [Synonyms]
AG 1295
NSC 380341
AG 1295 USP/EP/BP
TYROPHOSTIN AG1295
TYRPHOSTIN AG 1295
AG-1295
(NSC 380341
TYRPHOSTIN AG 1295, 99+%
AG 1295 PLATELET-DERIVED GROW
6,7-DIMETHYL-2-PHENYLQUINOXALINE
Quinoxaline, 6,7-dimethyl-2-phenyl- | [Molecular Formula]
C16H14N2 | [MDL Number]
MFCD00270912 | [MOL File]
71897-07-9.mol | [Molecular Weight]
234.3 |
| Chemical Properties | Back Directory | [Melting point ]
121 °C | [Boiling point ]
398.3±37.0 °C(Predicted) | [density ]
1.127±0.06 g/cm3(Predicted) | [storage temp. ]
−20°C
| [solubility ]
Chloroform (Slightly), Ethyl Acetate (Slightly) | [form ]
White solid | [pka]
1.29±0.30(Predicted) | [color ]
Yellow |
| 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. AG-1295 is a quinoxaline-type tyrphostin that acts as a potent and selective inhibitor of PDGF receptor kinase in vitro and in Swiss 3T3 cells (IC50s range from 0.3-1 μM). It inhibits PDGF-stimulated DNA synthesis with an IC50 value of 2.5 μM without affecting activity of the EGF receptor. | [Uses]
AG-1295 is a protein tyrosine kinase inhibitor. Antiproliferative agent used in the treatment of atherosclerosis, pulmonary fibrosis, and gliomas.
| [Definition]
ChEBI: 6,7-dimethyl-2-phenylquinoxaline is a quinoxaline derivative. It has a role as a geroprotector. | [in vitro]
the previous study investigated the effect of pdgf receptor-beta (pdgfr-β) inhibition by ag-1295 on the osteogenic differentiation of the mouse pre-osteoblastic cell line mc3t3-e1. results showed that ag-1295 could significantly increase the alkaline phosphatase (alp) activity and enhance the formation of mineralized nodules dose-dependently. moreover, the treatment with ag-1295 led to the up-regulated mrna expression of the osteogenic marker genes collagen type i, runt-related transcription factor 2, osterix, tissue-nonspecific alkaline phosphatase, as well as osteocalcin. consistent with its effect on osteoblast differentiation, ag-1295 was also able to significantly suppress the phosphorylation of erk1/2 in mc3t3-e1 cells [1]. | [in vivo]
a previous animal study was designed to evaluated the possible effects of ag1295 on the development of interstitial fibrosis in rats with unilateral ureteral obstruction, monitored by ed-a+ fibronectin expression, the number of macrophages. results showed that the i.p.treatment with ag1295 at 12 mg/kg could significantly reduce interstitial fibrosis as verified by a smaller sirius-red stained area and also by a reduced number of macrophages, and by the ed-a+ fibronectin deposition and the number of cells positive for α-smooth muscle actin [2]. | [IC 50]
0.3-1 μm for pdgf receptor kinase in vitro and in swiss 3t3 cells | [References]
[1] zhang yy, cui yz, luan j, zhou xy, zhang gl, han jx. platelet-derived growth factor receptor kinase inhibitor ag-1295 promotes osteoblast differentiation in mc3t3-e1 cells via the erk pathway. biosci trends. 2012 jun;6(3):130-5.
[2] ludewig d, kosmehl h, sommer m, bhmer fd, stein g. pdgf receptor kinase blocker ag1295 attenuates interstitial fibrosis in rat kidney after unilateral obstruction. cell tissue res. 2000 jan;299(1):97-103. |
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| Company Name: |
Spectrum Chemical Manufacturing Corp.
|
| Tel: |
021-021-021-67601398-809-809-809 15221380277 |
| Website: |
www.spectrumchemical.com/oa_html/index.jsp?minisite=10020&respid=22372&language=us |
| Company Name: |
Struchem Co., Ltd.
|
| Tel: |
0512-0512-63009836 15365350169 |
| Website: |
http://www.struchem.com |
|