TG 100572 - CAS 867334-05-2
Catalog number: B0084-429717
Category: Inhibitor
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TG 100572 is a multi-targeted kinase inhibitor that inhibits select growth factor receptor tyrosine kinases and Src familt kinases.
TG 100572; TG100572; TG-10057
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1.Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema.
Doukas J;Mahesh S;Umeda N;Kachi S;Akiyama H;Yokoi K;Cao J;Chen Z;Dellamary L;Tam B;Racanelli-Layton A;Hood J;Martin M;Noronha G;Soll R;Campochiaro PA J Cell Physiol. 2008 Jul;216(1):29-37. doi: 10.1002/jcp.21426.
Age-related macular degeneration, diabetic retinopathy, and retinal vein occlusions are complicated by neovascularization and macular edema. Multi-targeted kinase inhibitors that inhibit select growth factor receptor tyrosine kinases and/or components of their down-stream signaling cascades (such as Src kinases) are rationale treatment strategies for these disease processes. We describe the discovery and characterization of two such agents. TG100572, which inhibits Src kinases and selected receptor tyrosine kinases, induced apoptosis of proliferating endothelial cells in vitro. Systemic delivery of TG100572 in a murine model of laser-induced choroidal neovascularization (CNV) caused significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity. To minimize systemic exposure, topical delivery of TG100572 to the cornea was explored, and while substantial levels of TG100572 were achieved in the retina and choroid, superior exposure levels were achieved using TG100801, an inactive prodrug that generates TG100572 by de-esterification. Neither TG100801 nor TG100572 were detectable in plasma following topical delivery of TG100801, and adverse safety signals (such as weight loss) were not observed even with prolonged dosing schedules.
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CAS 867334-05-2 TG 100572

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