TG-100572 HCl | Multi-kinase inhibitor

TG100572 chemical structure

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TG-100572 (867331-64-4) is a multi-targeted kinase inhibitor which inhibits selected receptor kinases and Src kinases. IC50s = 2, 7, 2, 16, 13 VEGFR1, VEGFR2, FGFR1, FGFR2 PDGFRβ and  5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for Fgr, Fyn, Hck, Lck, Lyn, Src and Yes respectively.1  It suppresses choroidal neovascularization and retinal edema1. Blocks angiogenesis caused by HSV infection in the mouse eye.2 A prodrug strategy has been employed for topically applied AMD treatment.3

References/Citations:

  1. Doukas et al. (2008), Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema; J. Cell Physiol.. 216 29
  2. Sharma et al. (2011), An anti-inflammatory role of VEGFR2/Src kinase inhibitor in herpes simplex virus 1-induced immunopathology; J. Virol. 85 5995
  3. Palanki et al. (2008), 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. 51 1546
867331-64-4, TG-100572, TG-100572 HCl. TG100572, TG-100572 supplier

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TG-100572 (867331-64-4) is a multi-targeted kinase inhibitor which inhibits selected receptor kinases and Src kinases. IC50s = 2, 7, 2, 16, 13 VEGFR1, VEGFR2, FGFR1, FGFR2 PDGFRβ and  5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for Fgr, Fyn, Hck, Lck, Lyn, Src and Yes respectively.1  It suppresses choroidal neovascularization and retinal edema1. Blocks angiogenesis caused by HSV infection in the mouse eye.2 A prodrug strategy has been employed for topically applied AMD treatment.3

References/Citations:

  1. Doukas et al. (2008), Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema; J. Cell Physiol.. 216 29
  2. Sharma et al. (2011), An anti-inflammatory role of VEGFR2/Src kinase inhibitor in herpes simplex virus 1-induced immunopathology; J. Virol. 85 5995
  3. Palanki et al. (2008), 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. 51 1546