XAV-939

Catalog No.S1180 Batch:S118006

Technical Data

Formula

C₁₄H₁₁F₃N₂OS

Molecular Weight

312.31

CAS No.

284028-89-3

Solubility (25°C)*

In vitro

DMSO

16 mg/mL (51.23 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]

In vivo

AV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition.

Protocol (from reference)

Cell Assay:^{^[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.
Animal Study:^{^[3]}	Animal Models Male Sprague-Dawley rats Dosages 3 mg/kg Administration i.p.

Cell Assay:^{^[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.

Animal Study:^{^[3]}

Animal Models
Male Sprague-Dawley rats
Dosages
3 mg/kg
Administration
i.p.

References

https://pubmed.ncbi.nlm.nih.gov/21037379/
https://pubmed.ncbi.nlm.nih.gov/19759537/
https://pubmed.ncbi.nlm.nih.gov/33128175/

Customer Product Validation

: Data from [ Nat Commun , 2014 , 5, 5455 ]

: Data from [ Dis Model Mech , 2014 , 7(10), 1193-203 ]

: , , Cancer Lett, 2017, 400:194-202

: , , Dr. Marco Quarta of Stanford University

Selleck's XAV-939 has been cited by 432 publications

A multi-kingdom genetic barcoding system for precise clone isolation [ Nat Biotechnol, 2025, 10.1038/s41587-025-02649-1]	PubMed: 40399693
Spatial covariance reveals isothiocyanate natural products adjust redox stress to restore function in alpha-1-antitrypsin deficiency [ Cell Rep Med, 2025, 6(1):101917]	PubMed: 39809267
Longitudinal pharmacogenomic analysis of refractory lung cancer to identify therapeutic candidates for epidermal growth factor receptor-tyrosine kinase inhibitor resistance subclones [ Exp Mol Med, 2025, 10.1038/s12276-025-01493-2]	PubMed: 40615564
Interferon-induced PARP14-mediated ADP-ribosylation in p62 bodies requires the ubiquitin-proteasome system [ EMBO J, 2025, 10.1038/s44318-025-00421-4]	PubMed: 40195501
Wnt signaling inhibits casein kinase 1α activity by modulating its interaction with protein phosphatase 2A [ Cell Rep, 2025, 44(2):115274]	PubMed: 39908140
Requirements for the neurodevelopmental disorder-associated gene ZNF292 in human cortical interneuron development and function [ Cell Rep, 2025, 44(5):115597]	PubMed: 40257863
Dedifferentiated fat cells-derived exosomes (DFATs-Exos) loaded in GelMA accelerated diabetic wound healing through Wnt/β-catenin pathway [ Stem Cell Res Ther, 2025, 16(1):103]	PubMed: 40022232
Modulating Wnt/β-catenin pathway activity to enhance chemosensitivity in cholangiocarcinoma [ Biomed Pharmacother, 2025, 188:118225]	PubMed: 40472719
Colorectal cancer cell line-derived organoid model with stem cell properties captures the regrowing state of residual cancer cells after neoadjuvant chemotherapy [ Cell Death Discov, 2025, 11(1):282]	PubMed: 40537472
Regulation of ER stress-induced apoptotic and inflammatory responses via YAP/TAZ-mediated control of the TRAIL-R2/DR5 signaling pathway [ Cell Death Discov, 2025, 11(1):42]	PubMed: 39904986

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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