For research use only. Not for therapeutic Use.
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[1][2][3][4].
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[1].
AG1295 (10 μM, 100 μM) significantly inhibits rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB in vitro[2].
AG-1295 reduces neointimal formation in aortic allograft vasculopathy by inhibition of PDGFR-beta-triggered tyrosine phosphorylation[3].
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[4].
Catalog Number | R017059 |
CAS Number | 71897-07-9 |
Synonyms | 6,7-dimethyl-2-phenylquinoxaline |
Molecular Formula | C16H14N2 |
Purity | ≥95% |
InChI | InChI=1S/C16H14N2/c1-11-8-14-15(9-12(11)2)18-16(10-17-14)13-6-4-3-5-7-13/h3-10H,1-2H3 |
InChIKey | FQNCLVJEQCJWSU-UHFFFAOYSA-N |
SMILES | CC1=CC2=NC=C(N=C2C=C1C)C3=CC=CC=C3 |
Reference | [1]. Kovalenko M, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1;54(23):6106-14. [2]. Zheng Y, et al. Platelet-derived growth factor receptor kinase inhibitor AG1295 and inhibition of experimental proliferative vitreoretinopathy. Jpn J Ophthalmol. 2003 Mar-Apr;47(2):158-65. [3]. Inhibition of aortic allograft vasculopathy by local delivery of platelet-derived growth factor receptor tyrosine-kinase blocker AG-1295. Transplantation. 2002 Nov 15;74(9):1335-41. [4]. Ludewig D, et al. PDGF receptor kinase blocker AG1295 attenuates interstitial fibrosis in rat kidney after unilateral obstruction. Cell Tissue Res. 2000 Jan;299(1):97-103. |