TG100572

TG100572 is a potent small molecule multi-targeted kinase inhibitor that inhibits both receptor tyrosine kinases and Src family kinases. It demonstrates sub-nanomolar to low nanomolar inhibitory activity against several key targets including VEGFR1 (IC50 = 2 nM), VEGFR2 (7 nM), FGFR1 (2 nM), FGFR2 (16 nM), PDGFRβ (13 nM), Fgr (5 nM), Fyn (0.5 nM), Hck (6 nM), Lck (0.1 nM), Lyn (0.4 nM), Src (1 nM), and Yes kinase (0.2 nM)[1][5][8]. TG100572 blocks vascular endothelial growth factor-induced phosphorylation of downstream signaling molecules such as extracellular signal-regulated kinase and focal adhesion kinase, leading to inhibition of angiogenesis and vascular permeability[6]. It induces apoptosis in proliferating endothelial cells but not in quiescent cells[5][8]. Preclinical studies have shown efficacy in models of pathological ocular neovascularization such as age-related macular degeneration and diabetic retinopathy[6][9]. TG100801 is a prodrug of TG100572 designed for topical ocular delivery; after administration, it is converted into the active form within ocular tissues[9].

Other names

TG-100572 HClTG100572 HClTG 100572 HCl4-chloro-3-(5-methyl-3-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)amino)benzo[e][1,2,4]triazin-7-yl)phenol hydrochloride