AG 1295
AG 1295 Basic information
- Product Name:
- AG 1295
- Synonyms:
-
- 6,7-DIMETHYL-2-PHENYLQUINOXALINE
- AG 1295
- TYROPHOSTIN AG1295
- TYRPHOSTIN AG 1295
- AG 1295 PLATELET-DERIVED GROW
- TYRPHOSTIN AG 1295, 99+%
- Quinoxaline, 6,7-dimethyl-2-phenyl-
- AG-1295 (NSC 380341
- CAS:
- 71897-07-9
- MF:
- C16H14N2
- MW:
- 234.3
- Mol File:
- 71897-07-9.mol
AG 1295 Chemical Properties
- 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
Safety Information
- Safety Statements
- 22-24/25
- WGK Germany
- 3
MSDS
- Language:English Provider:SigmaAldrich
AG 1295 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-
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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