EW-7197

CAS No. 1352608-82-2

EW-7197( Vactosertib | EW7197 | TEW-7197 )

Catalog No. M11430 CAS No. 1352608-82-2

EW-7197 (Vactosertib, TEW-7197) is a highly potent, selective inhibitor of TGF-β type I receptor kinase (ALK5) with IC50 of 11 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 35 In Stock
5MG 58 In Stock
10MG 87 In Stock
25MG 147 In Stock
50MG 230 In Stock
100MG 354 In Stock
200MG 524 In Stock
500MG 822 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    EW-7197
  • Note
    Research use only, not for human use.
  • Brief Description
    EW-7197 (Vactosertib, TEW-7197) is a highly potent, selective inhibitor of TGF-β type I receptor kinase (ALK5) with IC50 of 11 nM.
  • Description
    EW-7197 (Vactosertib, TEW-7197) is a highly potent, selective inhibitor of TGF-β type I receptor kinase (ALK5) with IC50 of 11 nM; also inhibits ALK4 (IC50=13 nM) and shows less potency for p38α (IC50=280 nM); exhibits no inhibition on ALK1/2/3/6 (>10 uM); inhibits Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice and 4T1 orthotopic-grafted mice; oral bioavailability (Hcl salt).Blood Cancer Phase 1 Clinical(In Vitro):Vactosertib (10-1000 nM; 30 minutes; 4T1 cells) treatment blocks the TGFβ-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner in 4T1 cells.Vactosertib suppresses the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells. The IC50 value of Vactosertib on pSmad3 in 4T1 cells is 10-30 nM.Vactosertib abrogates TGFb1-induced tumor cell migration and invasion.TGFβ1 downregulated the mRNA level of CDH1 and upregulated the mRNA levels of FN1, HMGA2 (high-mobility group AT-hook 2), SNAI1, and SNAI2 (Snail family zinc finger 1 and 2, respectively). Moreover, Vactosertib abolishes the TGFβ1-induced effects on genes related to epithelial-to-mesenchymal transition (EMT).(In Vivo):Vactosertib (40 mg/kg; intraperitoneal injection; every other day; for 10 weeks; MMTV/c-Neu female mice) treatment inhibits Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice.Vactosertib also inhibits the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Furthermore, Vactosertib enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice.
  • In Vitro
    Western Blot Analysis Cell Line:4T1 cells Concentration:10 nM, 30 μM, 50 nM, 100 μM, 300 nM, 500 nM, 1000 nM.Incubation Time:30 minutes Result:Blocked the TGFb-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner.
  • In Vivo
    Animal Model:Mammary tumor virus (MMTV)/c-Neu female mice (32-week-old) Dosage:40 mg/kg Administration:Intraperitoneal injection; every other day; for 10 weeks Result:Inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice.
  • Synonyms
    Vactosertib | EW7197 | TEW-7197
  • Pathway
    TGF-beta/Smad
  • Target
    TGFBR
  • Recptor
    ALK1|ALK2|ALK3|ALK4|ALK5
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1352608-82-2
  • Formula Weight
    399.4236
  • Molecular Formula
    C22H18FN7
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    FC1=CC=CC=C1NCC2=NC(C3=CN4C(C=C3)=NC=N4)=C(C5=NC(C)=CC=C5)N2
  • Chemical Name
    1H-Imidazole-2-methanamine,N-(2-fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Jin CH, et al. J Med Chem. 2014 May 22;57(10):4213-38. 2. Son JY, et al. Mol Cancer Ther. 2014 Jul;13(7):1704-16. 3. Yoon JH, et al. EMBO Mol Med. 2013 Nov;5(11):1720-39.
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