EW-7197 | ALK4/5 inhibitor

CAS:
 1352608-82-2
Catalog Number:
 10-4989
EW-7197 chemical structure

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EW-7197 (1352608-82-2) is a potent (IC50 = 13 nM ALK4, 11 nM ALK5 HotSpot assay) and selective inhibitor of ALK4/5.1 It increased CD3+, IFN+CD8+, and NK cells and decreased myeloid suppressor cells in a mouse model of osteosarcoma.2 EW-7197 suppressed the epithelial-mesenchymal transition in various cancer models.3-5 It synergized with pomalidomide to increase T-cell fitness in a multiple myeloma model.6 EW-7197 displayed therapeutic effects in various models of fibrosis.7,8

References/Citations:

  1. Jin et al. (2014), Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridine-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-beta type I receptor kinase as cancer immunotherapy/antifibrotic agent; J. Med. Chem. 57 4213
  2. Choi et al. (2024); Oral transforming growth factor-beta receptor 1 inhibitor vactosertib promotes osteosarcoma regression by targeting tumor proliferation and enhancing anti-tumor immunity, Cancer Commun. (Lond). 44 884
  3. Park et al. (2015); TIMP-1 mediates TGF-ß-dependent crosstalk between hepatic stellate and cancer cells via FAK signaling, Sci. Rep. 5 16492
  4. Park et al. (2015); Combinatorial TGF-ß attenuation with paclitaxel inhibits the epithelial-to-mesenchymal transition and breast cancer stem-like cells, Oncotarget 6 37526
  5. Kaowinn et al. (2017); Cancer upregulated gene 2 induces epithelial-mesenchymal transition of human lung cancer cells via TGF-ß signaling, Oncotarget 8 5092
  6. Malek et al. (2024); The TGFß type I receptor kinase inhibitor vactosertib in combination with pomalidomide in relapsed/refractory multiple myeloma: a phase 1b trial, Nat. Commun. 15 7388
  7. Park et al. (2015); EW-7197 inhibits hepatic, renal, and pulmonary fibrosis by blocking TGF-beta/Smad and ROS signaling, Cell Mol. Life Sci. 72 2023
  8. Boonloh et al. (2025); Combination of THU/ALK-5i exhibits profound anti-MASH activity through suppression of lipogenesis and fibrogenesis, Sci. Rep. 15 39936
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CAS:
1352608-82-2
Catalog Number:
10-4989
Activity:
ALK4/5 inhibitor
Chemical Names:
2-Fluoro-N-[[5-(6-methyl-2-pyridinyl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-1H-imidazol-2-yl]methyl]aniline
Alternate Name:
Vactosertib
Molecular Weight:
399.43
Molecular Formula:

C22H18FN7

Solubility:
Soluble in DMSO (>50 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

EW-7197 (1352608-82-2) is a potent (IC50 = 13 nM ALK4, 11 nM ALK5 HotSpot assay) and selective inhibitor of ALK4/5.1 It increased CD3+, IFN+CD8+, and NK cells and decreased myeloid suppressor cells in a mouse model of osteosarcoma.2 EW-7197 suppressed the epithelial-mesenchymal transition in various cancer models.3-5 It synergized with pomalidomide to increase T-cell fitness in a multiple myeloma model.6 EW-7197 displayed therapeutic effects in various models of fibrosis.7,8

References/Citations:

  1. Jin et al. (2014), Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridine-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-beta type I receptor kinase as cancer immunotherapy/antifibrotic agent; J. Med. Chem. 57 4213
  2. Choi et al. (2024); Oral transforming growth factor-beta receptor 1 inhibitor vactosertib promotes osteosarcoma regression by targeting tumor proliferation and enhancing anti-tumor immunity, Cancer Commun. (Lond). 44 884
  3. Park et al. (2015); TIMP-1 mediates TGF-ß-dependent crosstalk between hepatic stellate and cancer cells via FAK signaling, Sci. Rep. 5 16492
  4. Park et al. (2015); Combinatorial TGF-ß attenuation with paclitaxel inhibits the epithelial-to-mesenchymal transition and breast cancer stem-like cells, Oncotarget 6 37526
  5. Kaowinn et al. (2017); Cancer upregulated gene 2 induces epithelial-mesenchymal transition of human lung cancer cells via TGF-ß signaling, Oncotarget 8 5092
  6. Malek et al. (2024); The TGFß type I receptor kinase inhibitor vactosertib in combination with pomalidomide in relapsed/refractory multiple myeloma: a phase 1b trial, Nat. Commun. 15 7388
  7. Park et al. (2015); EW-7197 inhibits hepatic, renal, and pulmonary fibrosis by blocking TGF-beta/Smad and ROS signaling, Cell Mol. Life Sci. 72 2023
  8. Boonloh et al. (2025); Combination of THU/ALK-5i exhibits profound anti-MASH activity through suppression of lipogenesis and fibrogenesis, Sci. Rep. 15 39936

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