Uses
TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
Biological Activity
tg100801 is a multi-kinases inhibitor. it is a pro-drug version of tg100572. [1]tg100572 inhibits several growth factor receptors in addition to src family kinases. tg100801 significantly inhibited laser-induced cnv in mice, and suppressed fluorescein leakage from the vasculature and retinal thickening measured by optical coherence tomography in a rat model or retinal vein occlusion. tg100801 may play as a new topically applied treatment approach for ocular neovascularization and retinal edema. the highest concentration of tg100801 was found at the front of the rat eye (conjunctiva and cornea). [1]
References
1. doukas j, mahesh s, umeda n et al. topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. j cell physiol. 2008 jul;216(1):29-37.
