XAV-939 | CAS#284028-89-3 | TNKS Inhibitor

MedKoo Cat#: 406134 | Name: XAV-939

Description:

WARNING: This product is for research use only, not for human or veterinary use.

XAV-939 is a Tankyrase (TNKS) inhibitor with potential anticancer activity. XAV-939 antagonizes Wnt signaling via stimulation of β-catenin degradation and stabilization of axin. XAV-939 inhibits proliferation of the μ-catenin-dependent colon carcinoma cell line DLD-1. Promotes cardiomyogenic development in mesoderm progenitor cells.

Chemical Structure

XAV-939

CAS#284028-89-3

Theoretical Analysis

MedKoo Cat#: 406134

Name: XAV-939

CAS#: 284028-89-3

Chemical Formula: C14H11F3N2OS

Exact Mass: 312.0544

Molecular Weight: 312.31

Elemental Analysis: C, 53.84; H, 3.55; F, 18.25; N, 8.97; O, 5.12; S, 10.27

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,650.00	Ready to ship

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Related CAS #

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Synonym

XAV939; XAV 939; XAV-939.

IUPAC/Chemical Name

2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-3H-thiopyrano[4,3-d]pyrimidin-4(5H)-one

InChi Key

KLGQSVMIPOVQAX-UHFFFAOYSA-N

InChi Code

InChI=1S/C14H11F3N2OS/c15-14(16,17)9-3-1-8(2-4-9)12-18-11-5-6-21-7-10(11)13(20)19-12/h1-4H,5-7H2,(H,18,19,20)

SMILES Code

O=C1C(CSCC2)=C2N=C(C3=CC=C(C(F)(F)F)C=C3)N1

Appearance

White Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>5 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#BBC61101

QC Data

View QC data: current batch, Lot#BBC61101

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

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.

In vitro activity:

Calcification of human VIC cultures was induced by cultivation in an osteogenic medium and the effect of co-incubation with 1μM XAV-939 was monitored. Calcification was quantified when mineral deposits were visible in culture and was histologically verified by von Kossa or Alizarin red staining and by IR-spectroscopy. Protein expression of alkaline phosphatase, Axin, β-catenin and Sox9 were quantified by western blotting. In 58% of the VIC preparations, calcification was induced in an osteogenic culture medium and was accompanied by upregulation of alkaline phosphatase. The calcification induction was prevented by the XAV-939 co-treatment and the alkaline phosphatase upregulation was suppressed. As expected, Axin was upregulated, but the levels of active non-phospho-β-catenin were also enhanced. Sox9 was induced during XAV-939 treatment but apparently not as a result of downregulation of β-catenin signalling. XAV-939 was therefore able to prevent calcification of human VIC cultures, and XAV-939 treatment was accompanied by upregulation of active non-phospho-β-catenin. Although XAV-939 does not downregulate active β-catenin, treatment with XAV-939 results in Sox9 upregulation that may prevent the calcification process. Reference: PLoS One. 2018 Dec 7;13(12):e0208774. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/30532256/

In vivo activity:

Mice underwent destabilization of the medial meniscus surgery and were treated by intra-articular injection with XAV-939, a small-molecule inhibitor of Wnt/β-catenin signaling. Wnt/β-catenin signaling was highly activated in murine synovial fibroblasts as well as in OA-derived human synovial fibroblasts. XAV-939 ameliorated OA severity associated with reduced cartilage degeneration and synovitis in vivo. Wnt inhibition using XAV-939 attenuated the proliferation and type I collagen synthesis in synovial fibroblasts in vitro but did not affect human OA-derived chondrocyte proliferation. However, Wnt modulation increased COL2A1 and PRG4 transcripts, which are downregulated in chondrocytes in OA. I Reference: JCI Insight. 2018 Feb 8;3(3):e96308. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/29415892/

	Solvent	mg/mL	mM
Solubility
	DMSO	10.4	33.36

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 312.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

In vitro protocol:

1. Dittfeld C, Reimann G, Mieting A, Büttner P, Jannasch A, Plötze K, Steiner G, Tugtekin SM, Matschke K. Treatment with XAV-939 prevents in vitro calcification of human valvular interstitial cells. PLoS One. 2018 Dec 7;13(12):e0208774. doi: 10.1371/journal.pone.0208774. PMID: 30532256; PMCID: PMC6286025. 2. Almasoud N, Binhamdan S, Younis G, Alaskar H, Alotaibi A, Manikandan M, Alfayez M, Kassem M, AlMuraikhi N. Tankyrase inhibitor XAV-939 enhances osteoblastogenesis and mineralization of human skeletal (mesenchymal) stem cells. Sci Rep. 2020 Oct 7;10(1):16746. doi: 10.1038/s41598-020-73439-9. Erratum in: Sci Rep. 2021 Feb 19;11(1):4559. PMID: 33028869; PMCID: PMC7541626.

In vivo protocol:

1. Lietman C, Wu B, Lechner S, Shinar A, Sehgal M, Rossomacha E, Datta P, Sharma A, Gandhi R, Kapoor M, Young PP. Inhibition of Wnt/β-catenin signaling ameliorates osteoarthritis in a murine model of experimental osteoarthritis. JCI Insight. 2018 Feb 8;3(3):e96308. doi: 10.1172/jci.insight.96308. PMID: 29415892; PMCID: PMC5821202.

1: Chugh RM, Bhanja P, Zitter R, Gunewardena S, Badkul R, Saha S. Modulation of β-Catenin promotes WNT expression in macrophages and mitigates intestinal injury. Cell Commun Signal. 2025 Feb 11;23(1):78. doi: 10.1186/s12964-025-02065-7. PMID: 39934819; PMCID: PMC11818365. 2: Sun T, Ma D, Song Y, Hu J, Yang Z, Wang X, Zhang J. Effects of 0.01 mM strontium on human periodontal ligament stem cell osteogenic differentiation via the Wnt/β-catenin signaling pathway. J Int Med Res. 2025 Feb;53(2):3000605251315024. doi: 10.1177/03000605251315024. PMID: 39932304; PMCID: PMC11815949. 3: Chen Y, Shi H, Dong Y, Cui W. LncRNA MSTO2P affects the proliferation, invasion and migration of non-small cell lung cancer by regulating the Wnt/β-catenin pathway. Discov Oncol. 2025 Feb 10;16(1):150. doi: 10.1007/s12672-025-01920-w. PMID: 39928213; PMCID: PMC11811353. 4: Kamaly NA, Kamel AS, Sadik NA, Shahin NN. Milnacipran and Vanillin Alleviate Fibromyalgia-Associated Depression in Reserpine-Induced Rat Model: Role of Wnt/β-Catenin Signaling. Mol Neurobiol. 2025 Feb 10. doi: 10.1007/s12035-025-04723-w. Epub ahead of print. PMID: 39924579. 5: He H, Yuan X, Chen Y, Hu T, Cheng B, Du R, Huang J, Geng X, Li H, Liu S, Liu Z. Semaphorin 3A Confers Protection against Oxidative Stress-induced Damage in Periodontal Ligament Stem Cells through the Activation of the Wnt/β-catenin Signaling Pathway. Curr Stem Cell Res Ther. 2025 Jan 17. doi: 10.2174/011574888X343230250107145153. Epub ahead of print. PMID: 39871562. 6: Ichisaka Y, Takei C, Naito K, Higa M, Yano S, Niwa T, Shimizu H. The Role of Indoxyl Sulfate in Exacerbating Colorectal Cancer During Chronic Kidney Disease Progression: Insights into the Akt/β-Catenin/c-Myc and AhR/c-Myc Pathways in HCT-116 Colorectal Cancer Cells. Toxins (Basel). 2025 Jan 1;17(1):17. doi: 10.3390/toxins17010017. PMID: 39852970; PMCID: PMC11769072. 7: Li S, Yang K, Ye J, Xu C, Qin Z, Chen Y, Yu L, Zhou T, Sun B, Xu J. LGALS4 inhibits glycolysis and promotes apoptosis of colorectal cancer cells via β‑catenin signaling. Oncol Lett. 2025 Jan 7;29(3):126. doi: 10.3892/ol.2025.14873. PMID: 39807100; PMCID: PMC11726281. 8: Ming H, Scatolin GN, Ojeda A, Jiang Z. Establishment of bovine extraembryonic endoderm cells. bioRxiv [Preprint]. 2024 Dec 17:2024.12.17.628911. doi: 10.1101/2024.12.17.628911. PMID: 39763779; PMCID: PMC11702706. 9: Shen Y, Wang J, Dai Y, Wan X, Zhang J, Le Q. RSPO3 Promotes Proliferation and Self-Renewal of Limbal Epithelial Stem Cells Through a WNT/β-Catenin-Independent Signaling Pathway. Invest Ophthalmol Vis Sci. 2025 Jan 2;66(1):8. doi: 10.1167/iovs.66.1.8. PMID: 39760688; PMCID: PMC11717127. 10: Wang MN, Zuo GY, Wang X, Han Y, Xia CY, Pan CH, Guo YX, Wang YM, Yang H, Zhang WK, He J, Xu JK. Amelioration of gap junction dysfunction in a depression model by loganin: Involvement of GSK-3β/β-catenin signaling. J Ethnopharmacol. 2025 Feb 11;341:119288. doi: 10.1016/j.jep.2024.119288. Epub 2024 Dec 26. PMID: 39732296. 11: Fan G, Zhang C. FNDC1 Facilitates Proliferation, Migration, and Invasion of Breast Cancer Cells Through Modulating Wnt/β-Catenin Pathway. Biochem Genet. 2024 Dec 13. doi: 10.1007/s10528-024-10994-0. Epub ahead of print. PMID: 39671143. 12: Liang SJ, Wang K, Mao DB, Xie LW, Zhu DJ. Inhibition of the Wnt/β‑catenin signaling pathway and SOX9 by XAV939 did not alleviate inflammation in a dextran sulfate sodium‑induced ulcerative colitis model. Exp Ther Med. 2024 Nov 26;29(2):24. doi: 10.3892/etm.2024.12774. PMID: 39650775; PMCID: PMC11619566. 13: Hao SR, Xie ZF, Li JX, Wang QZ, Wu TT, Shen T, Wu QL. Butorphanol Alleviates Hypoxia/Reoxygenation-Induced Myocardial Injury by Activating Wnt/β-Catenin Signal Pathway. J Appl Toxicol. 2024 Dec 3. doi: 10.1002/jat.4736. Epub ahead of print. PMID: 39627005. 14: Zhang Y, Gu F, Liu Y, Sun Y, Zhang L, Lu D. ZEB2 reduction contributes to pre-eclampsia via Wnt/β-Catenin pathway. Cell Div. 2024 Nov 29;19(1):34. doi: 10.1186/s13008-024-00137-7. PMID: 39614362; PMCID: PMC11607827. 15: Tang Y, Liu J, Liu L. Angiotensin-converting Enzyme 2 Suppresses Pulmonary Fibrosis Associated with Wnt and TGF-β1 Signaling Pathways. Discov Med. 2024 Nov;36(190):2274-2286. doi: 10.24976/Discov.Med.202436190.209. PMID: 39600282. 16: Hu XX, Yin YC, Xu P, Wei M, Zhang W. Network toxicology and cell experiments reveal the mechanism of DEHP-induced diabetic nephropathy via Wnt signaling pathway. Toxicol Appl Pharmacol. 2024 Dec;493:117144. doi: 10.1016/j.taap.2024.117144. Epub 2024 Nov 6. PMID: 39515621. 17: Tang X, Zhu Y, Cao Z, Wang X, Cai X, Tang Y, Zhou J, Wu M, Zhen X, Ding L, Yan G, Wang H, Sun H, Jiang R. CDC42 deficiency leads to endometrial stromal cell senescence in recurrent implantation failure. Hum Reprod. 2024 Dec 1;39(12):2768-2784. doi: 10.1093/humrep/deae246. PMID: 39487595; PMCID: PMC11630066. 18: Deng Z, Long D, Li C, Liu H, Li W, Zhong Y, Mo X, Li R, Yang Z, Kang Y, Mao G. IRF1-mediated upregulation of PARP12 promotes cartilage degradation by inhibiting PINK1/Parkin dependent mitophagy through ISG15 attenuating ubiquitylation and SUMOylation of MFN1/2. Bone Res. 2024 Oct 28;12(1):63. doi: 10.1038/s41413-024-00363-3. PMID: 39465252; PMCID: PMC11514270. 19: Chen H, Qian W, Zhou R, Zhang X, Chen T, Su M, Ma Y. The effects of therapeutic hypothermia on the expression of DKK3 and myocardial ischemia- reperfusion injury. Int Immunopharmacol. 2024 Dec 25;143(Pt 2):113386. doi: 10.1016/j.intimp.2024.113386. Epub 2024 Oct 17. PMID: 39423658. 20: Mai Y, Jing Z, Sun P, Wang Y, Dong P, Liu J. TARDBP drives T-cell acute lymphoblastic leukemia progression by binding MDM2 mRNA, involving β-catenin pathway. FASEB J. 2024 Oct 31;38(20):e70110. doi: 10.1096/fj.202400557RR. PMID: 39417407.