
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)






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2MG | 35 | In Stock |
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5MG | 58 | In Stock |
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10MG | 87 | In Stock |
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25MG | 147 | In Stock |
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50MG | 230 | In Stock |
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100MG | 354 | In Stock |
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Biological Information
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Product NameEW-7197
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NoteResearch use only, not for human use.
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Brief DescriptionEW-7197 (Vactosertib, TEW-7197) is a highly potent, selective inhibitor of TGF-β type I receptor kinase (ALK5) with IC50 of 11 nM.
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DescriptionEW-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.
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In VitroWestern 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.
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In VivoAnimal 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.
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SynonymsVactosertib | EW7197 | TEW-7197
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PathwayTGF-beta/Smad
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TargetTGFBR
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RecptorALK1|ALK2|ALK3|ALK4|ALK5
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1352608-82-2
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Formula Weight399.4236
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Molecular FormulaC22H18FN7
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESFC1=CC=CC=C1NCC2=NC(C3=CN4C(C=C3)=NC=N4)=C(C5=NC(C)=CC=C5)N2
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Chemical Name1H-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
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Storage(-20℃)
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ShippingWith Ice Pack
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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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