A potent inhibitor of ALK5
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EW-7197

Item No. 19231

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2-fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazole-2-methanamine
CAS Number
1352608-82-2
Synonyms
  • Vactosertib
Molecular Formula
C22H18FN7
Formula Weight
399.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
229, 306 nm
SMILES
CC1=NC(C2=C(C(C=C3)=CN4C3=NC=N4)N=C(CNC5=CC=CC=C5F)N2)=CC=C1
InChi Code
InChI=1S/C22H18FN7/c1-14-5-4-8-18(27-14)22-21(15-9-10-20-25-13-26-30(20)12-15)28-19(29-22)11-24-17-7-3-2-6-16(17)23/h2-10,12-13,24H,11H2,1H3,(H,28,29)
InChi Key
FJCDSQATIJKQKA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $134

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    5 mg

    $253

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    10 mg

    $399

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    Product Description

    EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC50 = 12.9 nM).1,2 It also inhibits ALK2 and ALK4 at nanomolar concentrations.2 EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus/c-Neu mice and 4TI orthotopic-grafted mice.2 It also inhibits epithelial-to-mesenchymal transition (EMT) in TGF-β-treated breast cancer cells.2 EW-7197 is used to block TGF-β signaling and EMT in animal models of cancer and fibrosis.3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jin, C.H., Krishnaiah, M., Sreenu, D., et al. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): A highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J. Med. Chem. 57(10), 4213-4238 (2014).

    2. Son, J.Y., Park, S.-Y., Kim, S.-J., et al. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis. Mol. Cancer Ther. 13(7), 1704-1716 (2014).

    3. Kaowinn, S., Kim, J., Lee, J., et al. Cancer upregulated gene 2 induces epithelial-mesenchymal transition of human lung cancer cells via TGF-β signaling. Oncotarget 8(3), 5092-5110 (2017).

    4. Kim, M.-J., Park, S.-A., Kim, C.H., et al. TGF-β type I receptor kinase inhibitor EW-7197 suppresses cholestatic liver fibrosis by inhibiting HIF1α-induced epithelial mesenchymal transition. Cell Physiol. Biochem. 38(2), 571-588 (2016).

    5. Yoon, J.-H., Jung, S.M., Park, S.H., et al. Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes. EMBO Mol. Med. 5(11), 1720-1739 (2013).