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 (6)
Reviews
Literature
Pathways

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 20 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.

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 biological activity of the product.

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.

View Related Products by Product Action

View all TGF-β Receptor Inhibitors

Keywords: SD 208, SD 208 supplier, 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, 3269, Tocris Bioscience

6 Citations for SD 208

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

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

Wang et al (2012) Protons sensitize epithelial cells to mesenchymal transition. PLoS One 7 e41249 PMID: 22844446

Mukherjee et al (2012) Transforming growth factor-β evokes Ca2+ waves and enhances gene expression in human pulmonary fibroblasts. Am J Respir Cell Mol Biol 46 757 PMID: 22268139

Pavlides et al (2016) TGF-β activates APC through Cdh1 binding for Cks1 and Skp2 proteasomal destruction stabilizing p27kip1 for normal endometrial growth. Cell Cycle 15 931 PMID: 26963853

Seliger et al (2016) Metformin inhibits proliferation and migration of glioblastoma cells independently of TGF-β2. Cell Cycle 15 1755 PMID: 27163626

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


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Reviews for SD 208

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

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Kinases Product Listing

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Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Stem Cells

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for SD 208

TGF-β

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.