Vactosertib (TEW-7197)

For research use only.

Catalog No.S7530 Synonyms: EW-7197

10 publications

Vactosertib (TEW-7197) Chemical Structure

CAS No. 1352608-82-2

Vactosertib  (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.

Selleck's Vactosertib (TEW-7197) has been cited by 10 publications

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  • Representative immunofluorescent images of HuL6 cells treated with EW-7197, TGF-β1, both, or neither for 72 h. Scale bars, 20 μm.

    Lab Invest, 2017, 97(3):232-242. Vactosertib (TEW-7197) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Vactosertib  (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.
ALK5 [1]
(Cell-free assay)
ALK4 [1]
(Cell-free assay)
11 nM 13 nM
In vitro

In HaCaT (3TP-luc) and 4T1 (3TP-luc) stable cells, 12b potently inhibits the TGF-β1-induced luciferase reporter activity with IC50 of 16.5 and 12.1 nM, respectively. [1] EW-7197 inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 M{j0V2Z2dmO2aX;uJIF{e2G7 NF\1ZohKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IFHMT|Uh\XiycnXzd4VlKGmwIHnud4VkfCCVZkmgZ4VtdHNidYPpcoch[2G|ZXnuJIF{KHO3YoP0doF1\SCkeTDyZYRqd2m|b4TvdIlkKGG|c3H5MEBKSzVyIE2gNE4xODdizszNMi=> Mli0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OE[1PFUoRjJ2N{i2OVg2RC:jPh?=
Sf9 NULqc4JtTnWwY4Tpc44h[XO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEeVVD3meZNm\CCDTFu1JIV5eHKnc4Pl[EBqdiCVZkmgbY5{\WO2IHPlcIx{KHW|aX7nJINie2WrbjDhd{B{fWK|dILheIUh[nlicILvdJJq\XSjcomgdoFlcW:rc3;0c5Bq[yCycn;0[YlvKGurbnHz[UBie3OjeTygTWM2OCB;IECuNFA6PjdizszNMi=> NEjabXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkS4N|E6QCd-Mk[0PFMyQTh:L3G+
4T1 NVf2ZWQ5TnWwY4Tpc44h[XO|YYm= M1PhdFI1KGi{cx?= MlTuTY5pcWKrdHnvckBw\iCDTFu1JIlvKG2xdYPlJFRVOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHRITmKndHGxMYlv\HWlZXSgcJVkcW[ncnHz[UBi[3Srdnn0fUBi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOC5yMUKxJO69VS5? NXXTTok6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3PFY2QDVpPkK0O|g3PTh3PD;hQi=>
HaCaT NH;vSWJHfW6ldHnvckBie3OjeR?= NWL0cZdGOjRiaILz NGP2bIxKdmirYnn0bY9vKG:oIFHMT|UhcW5iaIXtZY4hUGGFYWSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCWR1\i[ZRiOS2rbnT1Z4VlKGy3Y3nm[ZJie2ViYXP0bZZqfHliYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OCB;IECuNFE3PSEQvF2u MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd6NkW4OUc,OjR5OE[1PFU9N2F-
HEK293 MX\GeY5kfGmxbjDhd5NigQ>? MWezJJRwKDVwNzDtbY5{ MkThTY5pcWKrdHnvckBw\iCqdX3hckBGWkdiY3jhco5mdCCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGGodHXyJFMhfG9iNT63JI1qdnNiYomge4hwdGVvY3XscEBx[XSlaDDjcIFueCC2ZXPocolyfWVuIFnDOVAhRSB|MT6wOEDPxE1w MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd6NkW4OUc,OjR5OE[1PFU9N2F-
B16 MXTBcpRqfHWvb4KgZZN{[Xl? MXyyMlUhdWdxa3e= MV3BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEMU[gZ4VtdHNiaX6gcY92e2ViYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZidIXtc5Ihfm:udX3lJIF1KDJwNTDt[{9s\yxicH:gdYQhemWuYYTpeoUhfG9idnXobYNt\S22cnXheIVlKGOxboTyc4w> MoTIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OE[1PFUoRjJ2N{i2OVg2RC:jPh?=
B16 NEP4VIdCdnSrdIXtc5Ih[XO|YYm= NFLFfFgzNjVibXevb4c> M3:wb2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFKxOkBk\WyuczDpckBud3W|ZTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIIT1cY9zKGe{b4f0bEBifCB{LkWgcYcwc2duIIDvJJFlKHKnbHH0bZZmKHSxII\lbIlkdGVvdILlZZRm\CClb370do9t MlnUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OE[1PFUoRjJ2N{i2OVg2RC:jPh?=
B16 NEDyS5RCdnSrdIXtc5Ih[XO|YYm= Mn7ENk42KG2pL3vn M{P4NmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFKxOkBk\WyuczDpckBud3W|ZTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHz5cZBpKG6xZHWgcYV1[XO2YYPpd{BifCB{LkWgcYcwc2duIIDvJJFlKHKnbHH0bZZmKHSxII\lbIlkdGVvdILlZZRm\CClb370do9t MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd6NkW4OUc,OjR5OE[1PFU9N2F-

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
α-CUG2 / α-E-cadherin / α-N-cadherin / α-vimentin ; 

PubMed: 27974707     

A549-CUG2 and BEAS-CUG2 cells were treated with EW-7197 at different doses (0.25, 0.5, 1.25 and 2.5 μM) for 24 h. Expression of CUG2, E-cadherin, N-cadherin, and vimentin was detected by immunoblotting.

α-p-Smad2 / α-Smad2/3 / α-Twist / α-Snail ; 

PubMed: 27974707     

Expression of phospho-Smad2, Smad2/3, Snail and Twist in A549-CUG2 and BEAS-CUG2 cells treated with EW-7197 was detected by immunoblotting after cellular fractionations. Sp1 and actin were used loading controls for nuclear and cytosolic extracts, respectively.

α-p-AKT / α-AKT / α-p-ERK / α-ERK / α-p-JNK / α-JNK / α-p-p38 / α-p38 ; 

PubMed: 27974707     

A549-CUG2 and BEAS-CUG2 cells were treated with EW-7197 at the dose (1.25 μM) for 24 h. Activation of Akt, ERK, JNK and p38 MAPK was examined by immunoblotting.

Smad2 / Smad3 ; 

PubMed: 31496148     

Representative fluorescent immunocytochemistry of primary human fibroblasts cells stained with antibodies against total Smad2/3. Nuclei was dyed using DNA dye, DAPI (4,6-diamidino-2-phenylindole). Scale bar indicates 100 μm.

In vivo In rats, EW-7197 shows an oral bioavailability of 51% with high systemic exposure (AUC) of 1426 ng×h/mL and maximum plasma concentration (Cmax) of 1620 ng/mL. EW-7197 also shows low toxicity on the cardiovascular system, central nervous system, and respiratory system. [1] In a mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. [2] EW-7197 enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. [3]


Kinase Assay:


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Protein Kinase Assay:

A radioisotopic protein kinase assay (HotSpot assay) is performed at Reaction Biology Corporation.
Cell Research:


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  • Cell lines: 4T1 and MCF10A cells
  • Concentrations: ~5 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are seeded in 96 well plate and treated with indicated concentrations of EW-7197 in 0.2% HI-FBS medium for 72 h. Cells are dried after incubation with 10% TCA in media. Then, cells are incubated with 0.4% SRB (Sulforhodamine B) in 1% acetic acid for 30 min. After washing with 1% glacial acetic acid, bounded dye is released in 10 mM Tris buffer (pH 10.5) for 30 min. Absorbance is measured at 570 nm.

    (Only for Reference)
Animal Research:


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  • Animal Models: Mouse B16 melanoma model
  • Dosages: 2.5 mg/kg daily
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (197.78 mM)
Water Insoluble
Ethanol ''43 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 399.42


CAS No. 1352608-82-2
Storage powder
in solvent
Synonyms EW-7197
Smiles CC1=NC(=CC=C1)C2=C(N=C(N2)CNC3=CC=CC=C3F)C4=CN5C(=NC=N5)C=C4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID