XAV-939

Catalog No.S1180 Synonyms: NVP-XAV939

For research use only.

XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

XAV-939 Chemical Structure

CAS No. 284028-89-3

Selleck's XAV-939 has been cited by 307 publications

Purity & Quality Control

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Biological Activity

Description XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
Targets
TNKS2 [1]
(Cell-free assay)
TNKS1 [1]
(Cell-free assay)
4 nM 11 nM
In vitro

XAV-939 specifically inhibits tankyrase PARP activity. XAV-939 dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 μM XAV-939 results in marked elevation of tankyrase 1 levels. [1] XAV-939 is axin stabilizing agent. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. XAV-939 deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf-21 Mn36T4lv[XOnIFHzd4F6 MV6xPE44PSEQvF2= NWjZUWRDPjBibXnu NX\vc2hETE2VTx?= NFTBcFVKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBVVkuVMjDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDBwMEC1N{DPxE1? MlPoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6N{m0N|EoRjJ|OEe5OFMyRC:jPh?=
HEK293T Mlf4SpVv[3Srb36gRZN{[Xl? MXrEUXNQ MX7Jcohq[mm2aX;uJI9nKFewdDDzbYdv[WyrbnegZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDmc5J{c2:uaX6tbY5lfWOnZDDjRW1RKHKnc4DvcpNmKGWuZX3lcpQh[WO2aY\heIlwdiC5aYToJGlEPTBib3[gNE4xPzhizszN MojLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6N{m0N|EoRjJ|OEe5OFMyRC:jPh?=
HEK293T MnrmSpVv[3Srb36gRZN{[Xl? MljMNVAh|ryP NHTuU|hFVVOR NI\lbHdKdmirYnn0bY9vKG:oIHLleIEu[2G|ZXnuMYRmeGWwZHXueEBk[W6xbnnjZYwhX262MzDwZZRpf2G7IIfpeIghUUN3MDDv[kAxNjB3MTFOwG0> NFHWUJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG5NVU2Pyd-MkKxPVE2PTd:L3G+
HEK293T MV\GeY5kfGmxbjDBd5NigQ>? MWmyOEBp Mmj3SG1UVw>? NX\yOHl4UW6qaXLpeIlwdiCxZjDtc5V{\SCZboSzRUB{cWewYXzpcochf2m2aDDJR|UxKG:oIECuNFc5KM7:TR?= MknCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkCyNFMoRjJ{Mk[wNlA{RC:jPh?=
SW480 MV;GeY5kfGmxbjDBd5NigQ>? NX;IWYlEOTBizszN NX6wSI9yOjRiaB?= MVjEUXNQ MmLlV5Ri[mmuaYrheIlwdiCxZjDBfIlvOiC5aYToJGVEPTBib3[gNE4{PzFizszN NWj2XXdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlAzODNpPkKyNlYxOjB|PD;hQi=>
HEK293T NGHLNYFHfW6ldHnvckBCe3OjeR?= M3vxR|UxKM7:TR?= MXnEUXNQ M3WyRWhieyCwbzDF[oZm[3Rib36g[o9ze2uxbHnuMYlv\HWlZXSgZ2FOWCC|aXfuZYxqdmdiaX6gbJVu[W5iSFXLNlk{XCClZXzsd{Bkd2W6cILld5NqdmdiQ2LF NYj1SoNIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlAzODNpPkKyNlYxOjB|PD;hQi=>
IEC-6 MmDISpVv[3Srb36gRZN{[Xl? NVPJ[Is6PiCq NETKUWtCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFLleIEu[2G2ZX7pck9VS0ZiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCZboStN4EucW6mdXPl[EBigGmwMjDlfJBz\XO|aX;uJJdqfGhiSVO1NEBw\iByLk[0JO69VQ>? NE[y[Gk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC2NFQ5QSd-MkSwOlA1QDl:L3G+
IEC-6 NH3EU2NHfW6ldHnvckBCe3OjeR?= MXe2JIg> NF7pe2lCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFLleIEu[2G2ZX7pck9VS0ZiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCZboStN4EucW6mdXPl[EBt\3J3IHX4dJJme3Orb36ge4l1cCCLQ{WwJI9nKDJwOTFOwG0> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB4MES4PUc,OjRyNkC0PFk9N2F-
DLD1 MXHGeY5kfGmxbjDBd5NigQ>? MUKyNEDPxE1? NEXPe|AzPCCq MoLtSG1UVw>? MkHFTY5pcWKrdHnvckBw\iC2YX7rfZJie2ViYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCWQ1[t[IVx\W6mZX70JJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eR?= MoX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3Mke3PVIoRjJ2NUK3O|kzRC:jPh?=
DLD1 NVzJXpdKS3m2b4TvfIlkKEG|c3H5 NYTRVFdYOjBizszN MlnjNVAh\A>? NX3TOZBCTE2VTx?= NWHwSFVwS3m2b4TvfIlkcXS7IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;u MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV{N{e5Nkc,OjR3Mke3PVI9N2F-
VERO M2DEWGZ2dmO2aX;uJGF{e2G7 MmjSNlUh|ryP Mo\3SG1UVw>? MW\EbZN1fXKkZYOgVGFTKGKnbISgd5lvfGinc3nzMEBi\m[nY4TpcochfGinIHHjeIlvKGO7dH;zb4Vt\XSxbjygZ4VtdCC|aHHw[UBidmRiY3XscEBi\Ginc3nvci=> M17mO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{OyPFQ2Lz5{NUOzNlg1PTxxYU6=
HeLa MlPESpVv[3Srb36gRZN{[Xl? M1;QN|ExKM7:TR?= NXfC[ZF6PDhiaB?= MYLS[YR2[3Srb36gc4Yh[3m2b4DsZZNucWNiZHnzeJJq[nW2aX;uJIFv\CCwdXPs[YFzKHS{YX7zcI9k[XSrb36gc4Yh|rJvY3H0[Y5qdg>? NV7sempIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlE1QTlpPkK1NFYyPDl7PD;hQi=>
SiHa MV3GeY5kfGmxbjDBd5NigQ>? M1TvWFExKM7:TR?= NFXadFk1QCCq MV7S[YR2[3Srb36gc4Yh[3m2b4DsZZNucWNiZHnzeJJq[nW2aX;uJIFv\CCwdXPs[YFzKHS{YX7zcI9k[XSrb36gc4Yh|rJvY3H0[Y5qdg>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4MUS5PUc,OjVyNkG0PVk9N2F-
HEK293 MXPGeY5kfGmxbjDhd5NigQ>? M1zPSWlvcGmkaYTpc44hd2ZiV17UN2Ehe2mpbnHsbY5oKGmwIFjFT|I6OyClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmgbY4heHKnc3XuZ4Uhd2ZiZn;yd4twdGmwLDDJR|UxKD1iMD6wO|gh|ryPLh?= NULMTZBiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFQ2PzRpPkKzPFQ1PTd2PD;hQi=>
DLD1 M3vheWZ2dmO2aX;uJIF{e2G7 NIj6e44zPCCqcoO= M3:5WWlvcGmkaYTpc44hd2ZidHHub5lz[XOnIHnuJIh2dWGwIFTMSFEh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIGfueEBi[3Srdnn0fUBi\nSncjCyOEBpenNiYomgWGNHNWy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OCB;IECuO|A4KM7:TT6= NWrkUmpZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPVk3QDNpPkK1Nlk6Pjh|PD;hQi=>
Sf21 M3W1T2Z2dmO2aX;uJIF{e2G7 MljRNkBpenN? MWjJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiR2PUMZRi\2enZDDoeY1idiCWTlvTMVIhMDh2OTD0c{AyOTZ4IILld4llfWW|KTDlfJBz\XO|ZXSgbY4hcW5iaX7z[YN1KHOoMkGgZ4VtdHNicILlbY5kfWKjdHXkJIZweiB{IHjyd{Bnd2yub4fl[EBjgSC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{whUUN3MDC9JFAvODF5IN88UU4> MmPWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzNkO1PFEoRjJ5MU[zOVgyRC:jPh?=
A673 MVzxTHRUKGG|c3H5 M2HSOZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NIrPNm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC MULxTHRUKGG|c3H5 MlrBdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= M{TlZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A549 NV[xXIp{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmrHO|IhcHK| NXjhSHNQT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOTJwMzFOwG0v MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl|NEKxPUc,Ojl7M{SyNVk9N2F-
Assay
Methods Test Index PMID
Western blot β-catenin / E-cadherin / N-cadherin ; β-catenin / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin 31060551 28177909
Immunofluorescence β-catenin / E-cadherin ; Actin / PAR ; Hes1 / β-catenin / p-STAT3 31060551 25332845 25061499

Protocol (from reference)

Cell Research:[1]
  • Cell lines: WTK1 lymphoblasts
  • Concentrations: 1.0 μM
  • Incubation Time: 8 hours
  • Method: XAV-939 is solubilized in DMSO at 55 °C to make a 10 mM stock solution which may be diluted later to a working concentration of 100 μM. WTK1 lymphoblasts treated with either DMSO or 1.0 μM XAV-939 for 8 hours are loaded into independent wells of a 4-20% gradient SDS-PAGE every 2 hours over the course of 6 hours. At each time point, DMSO and XAV-939 samples are loaded into wells immediately adjacent to the prior time point. The corresponding load times at 0, 2 and 4 hours results in total run times of 2, 4 and 6 hours respectively. The gel is analyzed via western blot for DNA-PKcs following completion of the final run time and is quantified after normalization to actin loading controls.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.

1mg/mL

Chemical Information

Molecular Weight 312.31
Formula

C14H11F3N2OS

CAS No. 284028-89-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

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mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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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Frequently Asked Questions

Question 1:
I want to inject XAV 939 (Cat # S1180) into mice through I.P. and just wonder what kind of solvent/solution I can use for this.

Answer:
S1180 XAV-939 can be dissolved in 4% DMSO+corn oil at 1 mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. You can sonicate and warm it in water bath at about 45 degree to help dissolving. Then dilute with corn oil.

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