A TGF-β type 1 receptor kinase inhibitor
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LY2157299

Item No. 15312

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide
CAS Number
700874-72-2
Synonyms
  • Galunisertib
Molecular Formula
C22H19N5O
Formula Weight
369.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.25 mg/ml
λmax
238, 282 nm
SMILES
NC(C1=CC(C(C2=C(CCC3)N3N=C2C4=NC(C)=CC=C4)=CC=N5)=C5C=C1)=O
InChi Code
InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28)
InChi Key
IVRXNBXKWIJUQB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $209

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    10 mg

    $341

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    50 mg

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    Product Description

    LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM).1 It has been used to study the role of TGF-β signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts.2 LY2157299 has also been shown to inhibit the migration and tumor growth of hepatocellular carcinoma cell lines by disrupting Smad-2 phosphorylation.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mundla, S.R. A pyridin quinolin substituted pyrrolo [1,2-B] pyrazole monohydrate as TGFβinhibitor. PCT/US2006/025377, 1-13 (2014).

    2. Bhola, N.E., Balko, J.M., Dugger, T.C., et al. TGF-β inhibition enhances chemotherapy action against triple-negative breast cancer. J. Clin. Invest. 123(3), 1348-1358 (2013).

    3. Dituri, F., Mazzocca, A., Peidrò, F.J., et al. Differential inhibition of the TGF-β signaling pathway in HCC cells using the small molecule inhibitor LY2157299 and the D10 monoclonal antibody against TGF-β receptor type II. PLoS One 8(6), e67109 (2013).