SD 208

Pricing Availability Delivery Time Qty
Cat.No. 3269 - SD 208 | C17H10ClFN6 | CAS No. 627536-09-8
Description: Potent ATP-competitive TGF-βRI inhibitor
Chemical Name: 2-(5-Chloro-2-fluorophenyl)-4-[(4-pyridyl)amino]pteridine
Purity: ≥98% (HPLC)
Datasheet
Citations (2)

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.

Compound Libraries

SD 208 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 352.75
Formula C17H10ClFN6
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 627536-09-8
PubChem ID 10316032
InChI Key BERLXWPRSBJFHO-UHFFFAOYSA-N
Smiles FC(C=CC(Cl)=C3)=C3C2=NC1=NC=CN=C1C(NC4=CC=NC=C4)=N2

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.05 20mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 352.75. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.83 mL 14.17 mL 28.35 mL
5 mM 0.57 mL 2.83 mL 5.67 mL
10 mM 0.28 mL 1.42 mL 2.83 mL
50 mM 0.06 mL 0.28 mL 0.57 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 reference for SD 208, please let us know.

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Keywords: Potent ATP-competitive TGF-βRI TGF-β TGF-betaRI TGFbRI TGFbR1 tgf-b1inhibitors inhibits Transforming Growth Factors Beta Receptors TGF-beta Serine/Threonine Kinases RSTKs SD208 TGF-beta Receptors

2 Citations for SD 208

Citations are publications that use Tocris products. Selected citations for SD 208 include:

Li and Gotlieb (2011) Transforming growth factor-β regulates the growth of valve interstitial cells in vitro. Am J Pathol 179 1746 PMID: 21851806

Nistala et al (2010) Differential effects of alendronate and losartan therapy on osteopenia and aortic aneurysm in mice with severe Marfan syndrome. PLoS One 19 4790 PMID: 20871099


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