A potent, selective inhibitor of TGF-βRI
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

SD 208

Item No. 16619

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-4-pteridinamine
CAS Number
627536-09-8
Synonyms
  • TGF-β RI Kinase Inhibitor V
Molecular Formula
C17H10ClFN6
Formula Weight
352.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.3 mg/ml
λmax
205, 258, 362 nm
SMILES
ClC1=CC=C(F)C(C2=NC(N=CC=N3)=C3C(NC4=CC=NC=C4)=N2)=C1
InChi Code
InChI=1S/C17H10ClFN6/c18-10-1-2-13(19)12(9-10)15-24-16-14(21-7-8-22-16)17(25-15)23-11-3-5-20-6-4-11/h1-9H,(H,20,22,23,24,25)
InChi Key
BERLXWPRSBJFHO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $41

    Add

    5 mg

    $119

    Add

    10 mg

    $196

    Add

    25 mg

    $437

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    TGF-β is a cell growth and differentiation factor that has roles in cancer, fibrosis, and numerous other pathologies.1,2 TGF-β signals through two receptor tyrosine kinases, TGF-βRI and TGF-βRII. SD 208 is a potent inhibitor of TGF-βRI kinase (EC50 = 48 nM) that has minimal or no effect at a variety of other tyrosine or serine/threonine kinases, including TGF-βRII kinase.3 It blocks both autocrine and paracrine TGF-β signaling in glioma cells, inhibiting TGF-β-induced migration and invasion without affecting viability or proliferation.3 SD 208 is orally bioavailable and prevents TGF-β-induced Smad phosphorylation in spleens and brains of mice.3 It improves survival in mice with xenografted glioma by heightening the immune response against tumor cells and reverses bronchial hyperresponsiveness to allergens in ovalbumin-exposed mice.3,4 SD 208 also suppresses TGF-β-induced differentiation of proliferating myofibroblasts and induces dedifferentiation in the absence of TGF-β.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fuxe, J., Vincent, T., and de Herreros, A.G. Transcriptional crosstalk between TGF-β and stem cell pathways in tumor cell invasion. Cell Cycle 9(12), 2363-2374 (2010).

    2. Distler, J.H.W., and Distler, O. Intracellular tyrosine kinases as novel targets for anti-fibrotic therapy in systemic sclerosis. Rheumatology 47(Suppl 5), 10-11 (2008).

    3. Uhl, M., Aulwurm, S., Wischhusen, J., et al. SD-208, a novel transforming growth factor β receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Cancer Res. 64(21), 7954-7961 (2004).

    4. Leung, S.Y., Niimi, A., Noble, A., et al. 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(2), 586-594 (2006).

    5. Driesen, R.B., Nagaraju, C.K., Abi-Char, J., et al. Reversible and irreversible differentiation of cardiac fibroblasts. Cardiovasc. Res. 101(3), 411-422 (2014).

    6. Kapoun, A.M., Gaspar, N.J., Wang, Y., et al. Transforming growth factor-β receptor type 1 (TGFβRI) kinase activity but not p38 activation is required for TGFβRI-induced myofibroblast differentiation and profibrotic gene expression. Mol. Pharmacol. 70(2), 518-531 (2006).