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XAV-939

Name: XAV-939
Brand: Selleck Chemicals
SKU: S1180
Rating: 5 (307 reviews)

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.

CAS No. 284028-89-3

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

Purity & Quality Control

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PARP Signaling Pathway Map

Biological Activity

Description

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-

Click to View More Cell Line Experimental Data

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.

References

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. Click to purchase: Corn Oil	1mg/mL

Chemical Information

Molecular Weight	312.31
Formula	C₁₄H₁₁F₃N₂OS
CAS No.	284028-89-3
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F

Download XAV-939 SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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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.
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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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