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.
IC50&Target
PDGFR
体外研究
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 in vitro.
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
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.
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.
分子式
C16H14N2
分子量
234.30
CAS号
71897-07-9
运输条件
Room temperature in continental US; may vary elsewhere.