ag 1295;AG-1295;6,7-dimethyl-2-phenylquinoxaline;2-phenyl-6,7-dimethylquinoxaline;6,7-Dimethyl-2-phenyl-chinoxalin;6,7-dimethyl-2-phenyl-quinoxaline;F1284-0835;TYRPHOSTIN AG 1295
Cas No.
71897-07-9
分子式
C16H14N2
分子量
234.30
包装储存
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
生物活性
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.
性状
Solid
IC50 & Target[1][2]
PDGFR
体外研究(In Vitro)
AG 1295 inhibits PDGFR autophosphorylation with IC50s of 0.3-0.5 μM and 0.5-1 μM for membrane autophosphorylation assays and Swiss 3T3 cells, respectively.
AG1295 (10 μM, 100 μM) significantly inhibits rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB 体外研究.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
Cell Line:
Rabbit conjunctival fibroblasts cells
Concentration:
1 μM, 10 μM, 100 μM
Incubation Time:
3 days
Result:
Inhibited rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB.
体内研究(In Vivo)
AG-1295 reduces neointimal formation in aortic allograft vasculopathy by inhibition of PDGFR-beta-triggered tyrosine phosphorylation.
AG1295 (12 mg/kg; i.p.; daily; for 14 or 21 days) significantly reduces 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 alpha-smooth muscle actin.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Sprague-Dawley rats (240-270 g)
Dosage:
12 mg/kg
Administration:
Intraperitoneal injection; daily; for 14 or 21 days
Result:
Attenuated interstitial fibrosis in rat kidney after unilateral obstruction.