SD 208

Cat. No. 3269

SD 208 C17H10ClFN6 [627536-09-8]

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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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Uhl et al (2004) 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. Cancer Res. 64 7954. PMID: 15520202.

Kapoun et al (2006) 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. Mol.Pharmacol. 70 518. PMID: 16707625.

Leung et al (2006) Effect of transforming growth factor-β receptor I kinase inhibitor 2,4-disubstituted pteridine (SD-208) in chronic allergic airway inflammation and remodeling. J.Pharmacol.Exp.Ther. 319 586. PMID: 16888081.

Manaenko et al (2014) Inhibition of transforming growth factor-β attenuates brain injury and neurological deficits in a rat model of germinal matrix hemorrhage. Stroke 45 828. PMID: 24425124.

If you know of a relevant citation for this product please let us know.

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Keywords: SD 208, supplier, Potent, ATP-competitive, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1inhibitors, Transforming, Growth, Factors, Beta, Receptors, TGF-beta, Serine/Threonine, Kinases, RSTKs, SD208, Tocris Bioscience, TGF-β Receptor Inhibitors

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