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Products Details
Product Description
– TG 100801 Hydrochloride 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 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
Web ID
– HY-10187
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C33H31Cl2N5O3
References
– [1]Palanki MS, 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.|[2]Doukas, John, 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.
CAS Number
– 1018069-81-2
Molecular Weight
– 616.54
SMILES
– O=C(C1=CC=CC=C1)OC2=CC=C(Cl)C(C3=CC(C)=C(N=C(NC(C=C4)=CC=C4OCCN5CCCC5)N=N6)C6=C3)=C2.Cl
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– DMSO : 5 mg/mL (ultrasonic)
Target
– FGFR;PDGFR;Src;VEGFR
Isoform
– FGFR1;FGFR2;PDGFRβ;VEGFR1/Flt-1;VEGFR2/KDR/Flk-1
Pathway
– Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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