Vactosertib (TEW-7197)

Catalog No.S7530 Synonyms: EW-7197

For research use only.

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.

Vactosertib (TEW-7197) Chemical Structure

CAS No. 1352608-82-2

Selleck's Vactosertib (TEW-7197) has been cited by 12 Publications

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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.
Targets
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 NGrpS5NHfW6ldHnvckBie3OjeR?= MkTxTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCDTFu1JIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KHW|aX7nJINie2WrbjDhd{B{fWK|dILheIUh[nlicnHkbY9qe2:2b4DpZ{Bie3OjeTygTWM2OCB;IECuNFA4KM7:TT6= MnvKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OE[1PFUoRjJ2N{i2OVg2RC:jPh?=
Sf9 M2DTcGZ2dmO2aX;uJIF{e2G7 NXLzd5R3UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDHV3Qu\nW|ZXSgRWxMPSCneIDy[ZN{\WRiaX6gV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yClYYPlbY4h[XNic4Xid5Rz[XSnIHL5JJBzd3C{aXX0ZZJ6KHKjZHnvbZNwfG:yaXOgdJJwfGWrbjDrbY5ie2ViYYPzZZktKEmFNUCgQUAxNjByOU[3JO69VS5? NWDiU4UzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0PFMyQThpPkK2OFg{OTl6PD;hQi=>
4T1 M2jnTWZ2dmO2aX;uJIF{e2G7 NGPub4YzPCCqcoO= MYnJcohq[mm2aX;uJI9nKEGOS{WgbY4hdW:3c3WgOHQyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gWGdH[mW2YUGtbY5lfWOnZDDseYNq\mW{YYPlJIFkfGm4aYT5JIFnfGW{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjBzMkGg{txONg>? NVnH[2ZDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3PFY2QDVpPkK0O|g3PTh3PD;hQi=>
HaCaT MYjGeY5kfGmxbjDhd5NigQ>? Mn7yNlQhcHK| M{fBfmlvcGmkaYTpc44hd2ZiQVzLOUBqdiCqdX3hckBJ[UOjVDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFSJRnLleIEyNWmwZIXj[YQhdHWlaX\ldoF{\SCjY4Tpeol1gSCjZoTldkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxKD1iMD6wNVY2KM7:TT6= NEeyUmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe4OlU5PSd-MkS3PFY2QDV:L3G+
HEK293 NF;xeoJHfW6ldHnvckBie3OjeR?= NFr5VHM{KHSxIEWuO{BucW6| M2jMW2lvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHPoZY5v\WxiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjZoTldkA{KHSxIEWuO{BucW6|IHL5JJdpd2ynLXPlcIwheGG2Y3igZ4xidXBidHXjbI5qeXWnLDDJR|UxKD1iM{GuNFQh|ryPLh?= NHi2[mY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe4OlU5PSd-MkS3PFY2QDV:L3G+
B16 MnnyRY51cXS3bX;yJIF{e2G7 MYGyMlUhdWdxa3e= MVXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEMU[gZ4VtdHNiaX6gcY92e2ViYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZidIXtc5Ihfm:udX3lJIF1KDJwNTDt[{9s\yxicH:gdYQhemWuYYTpeoUhfG9idnXobYNt\S22cnXheIVlKGOxboTyc4w> MonjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OE[1PFUoRjJ2N{i2OVg2RC:jPh?=
B16 MYTBcpRqfHWvb4KgZZN{[Xl? MlvDNk42KG2pL3vn NXK0RZk1SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhdW:3c3WgRlE3KGOnbHzzJIlvKG2xdYPlJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geJVud3JiZ4Lve5RpKGG2IEKuOUBu\y:tZzygdI8heWRicnXsZZRqfmVidH:geoVpcWOuZT30doVifGWmIHPvcpRzd2x? MnO0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OE[1PFUoRjJ2N{i2OVg2RC:jPh?=
B16 M{XvemFvfGm2dX3vdkBie3OjeR?= NEfkVo0zNjVibXevb4c> M2XtUWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFKxOkBk\WyuczDpckBud3W|ZTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHz5cZBpKG6xZHWgcYV1[XO2YYPpd{BifCB{LkWgcYcwc2duIIDvJJFlKHKnbHH0bZZmKHSxII\lbIlkdGVvdILlZZRm\CClb370do9t MlfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OE[1PFUoRjJ2N{i2OVg2RC:jPh?=
Assay
Methods Test Index PMID
Western blot α-CUG2 / α-E-cadherin / α-N-cadherin / α-vimentin ; α-p-Smad2 / α-Smad2/3 / α-Twist / α-Snail ; α-p-AKT / α-AKT / α-p-ERK / α-ERK / α-p-JNK / α-JNK / α-p-p38 / α-p38 27974707
Immunofluorescence Smad2 / Smad3 31496148
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]

Protocol (from reference)

Kinase Assay:

[1]

  • Protein Kinase Assay:

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

Cell Research:

[3]

  • 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:

[2]

  • 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):
1%cmc-na
For best results, use promptly after mixing.

10mg/mL

* 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
Formula

C22H18FN7

CAS No. 1352608-82-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC(=CC=C1)C2=C(N=C(N2)CNC3=CC=CC=C3F)C4=CN5C(=NC=N5)C=C4

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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