A dual inhibitor of TGF-β type 1/type II receptor kinases
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.

LY2109761

Item No. 15409

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[5,6-dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-quinoline
CAS Number
700874-71-1
Molecular Formula
C26H27N5O2
Formula Weight
441.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 0.1 mg/mlEthanol: 2 mg/ml
λmax
236 nm
SMILES
C12=NC=CC(C3=C(CCC4)N4N=C3C5=CC=CC=N5)=C1C=CC(OCCN6CCOCC6)=C2
InChi Code
InChI=1S/C26H27N5O2/c1-2-9-27-22(4-1)26-25(24-5-3-11-31(24)29-26)21-8-10-28-23-18-19(6-7-20(21)23)33-17-14-30-12-15-32-16-13-30/h1-2,4,6-10,18H,3,5,11-17H2
InChi Key
IHLVSLOZUHKNMQ-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

    $49

    Add

    5 mg

    $109

    Add

    10 mg

    $194

    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

    LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases (IC50 = 69 nM).1 It has been used to study the role of TGF-β signaling in tumor cell migration and metastasis in pancreatic tumor cell lines where 5 μM of the compound completely disrupts Smad-2 phosphorylation, an immediate downstream target of the kinase activity.2 It can also suppress radiation-induced inflammatory cytokine signaling and proangiogenic genes, including ID1, in human primary fibrobalsts.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, H.y., McMillen, W.T., Heap, C.R., et al. Optimization of a dihydropyrrolopyrazole series of transforming growth factor-β type I receptor kinase domain inhibitors: Discovery of an orally bioavailable transforming growth factor-β receptor type I inhibitor as antitumor agent. J. Med. Chem. 51(7), 2302-2306 (2008).

    2. Melisi, D., Ishiyama, S., Sclabas, G.M., et al. LY2109761, a novel transforming growth factorβreceptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol. Cancer Ther. 7(4), 829-840 (2008).

    3. Flechsig, P., Dadrich, M., Bickelhaupt, S., et al. LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-β and BMP-associated proinflammatory and proangiogenic signals. Clin. Cancer Res. 18(13), 3616-3627 (2012).