TG 100801

• CAT Number: I005219
• CAS Number: 867331-82-6
• Molecular Formula: C33H30ClN5O3
• Molecular Weight: 580.08
• Purity: ≥95%
• Synonyms: [4-chloro-3-[5-methyl-3-[4-(2-pyrrolidin-1-ylethoxy)anilino]-1,2,4-benzotriazin-7-yl]phenyl] benzoate
• Target: VEGFR
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C

TG 100801 is the prodrug of TG 100572 (HY-10184), TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM or VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.IC50 value:Target: Src familt kinase; VEGFRTG 100801 is currently in a clinical trial as a first in class, VEGFr2 targeting, topically applied compound for the treatment of AMD. The formation of new blood vessels (angiogenesis), blood vessel leakage, and inflammation contribute to the progression of the eye disease, age-related macular degeneration (AMD), which is the leading cause of irreversible, severe loss of vision in people 55 years of age and older in the developed world. TG100801 is a new drug that inhibits ocular angiogenesis, vascular leak, and inflammation in laboratory studies, and may have great utility in the treatment of diseases such as AMD.

Reference

[1]. Mousa, Shaker A.; Mousa, Shaymaa S. Current status of vascular endothelial growth factor inhibition in age-related macular degeneration. BioDrugs (2010), 24(3), 183-194.
[2]. Doukas, John; Mahesh, Sankaranarayana; Umeda, Naoyasu et al. Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema. Journal of Cellular Physiology (2008), 216(1), 29-37.
[3]. A Phase 1 Safety Study of TG100801 Eye Drops in Healthy Volunteers.
[4]. Palanki MS, Akiyama H, Campochiaro P et al. Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. J Med Chem. 2008 Mar 27;51(6):1546-59.
[5]. Chappelow AV, Kaiser PK. Neovascular age-related macular degeneration: potential therapies. Drugs. 2008;68(8):1029-36.