Catalog Number: 3269
Chemical Name: 2-(5-Chloro-2-fluorophenyl)-4-[(4-pyridyl)amino]pteridine
Biological Activity
Potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50 = 49 nM). Displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively. Exhibits anti-inflammatory and antitumor activity. Also promotes an antiglioma immune response. Ameliorates germinal matrix hemorrhage-induced neurological deficits in neonatal rats.
Technical Data
  • M.Wt:
    352.75
  • Formula:
    C17H10ClFN6
  • Solubility:
    Soluble to 20 mM in DMSO with gentle warming
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    627536-09-8
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. SD-208, a novel transforming growth factor β feceptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogeneicity of murine and human glioma cells in vitro and in vivo.
    Uhl et al.
    Cancer Res., 2004;64:7954
  2. Transforming growth factor-β receptor type I receptor (TGFβRI) kinase activity but not p38 activation is required for TGFβRI-induced myofibroblast differentiation and profibrotic gene expression.
    Kapoun et al.
    Mol.Pharmacol., 2006;70:518
  3. Effect of transforming growth factor-β receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling.
    Leung et al.
    J.Pharmacol.Exp.Ther., 2006;319:586
  4. Inhibition of transforming growth factor-β attenuates brain injury and neurological deficits in a rat model of germinal matrix hemorrhage.
    Manaenko et al.
    Stroke, 2014;45:828
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SD 208 include:

2 Citations: Showing 1 - 2
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  1. Transforming growth factor-β regulates the growth of valve interstitial cells in vitro.
    Authors: Li and Gotlieb
    Am J Pathol 2011;179:1746
  2. Differential effects of alendronate and losartan therapy on osteopenia and aortic aneurysm in mice with severe Marfan syndrome.
    Authors: Nistala Et al.
    PLoS One 2010;19:4790

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