Name: XAV-939
Brand: Selleck Chemicals
SKU: S1180
Availability: InStock
Rating: 5 (425 reviews)

Jump to

Quality Control

Batch: Purity: 99.95%

99.95

Products Often Used Together with XAV-939

SU 5402

It promotes anterior central nervous system identity, while SU5402 accelerates hPSC differentiation toward neuroectodermal lineages.

LDN-193189

It and LDN-193189 are the least effective in improving the morphology of low-density P0 RPE cultures to varying extents.

SB431542

It and SB431542 significantly suppress MSC gene expression.

ICG-001

It and ICG-001 decrease the proliferation of the IGROV1 and SKOV3 ovarian cancer cell lines.

Related Targets	JAK TGF-beta/Smad Wnt/beta-catenin ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT
Other PARP Inhibitors	AZD5305 (Saruparib) Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) Pamiparib G007-LK UPF 1069 A-966492 Stenoparib (E7449)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Sf-21	Kinase Assay	18.75 μM	60 min	DMSO	Inhibition of N-terminal GST-tagged TNKS2 expressed with IC50 of 0.0053 μM	23879431
HEK293T	Function Assay			DMSO	Inhibition of Wnt signaling assessed as inhibition of forskolin-induced cAMP response element activation with IC50 of 0.078 μM	23879431
HEK293T	Function Assay	10 μM		DMSO	Inhibition of beta-casein-dependent canonical Wnt3 pathway with IC50 of 0.051 μM	22191557
HEK293T	Function Assay		24 h	DMSO	Inhibition of mouse Wnt3A signaling with IC50 of 0.078 μM	22260203
SW480	Function Assay	10 μM	24 h	DMSO	Stabilization of Axin2 with EC50 of 0.371 μM	22260203
HEK293T	Function Assay	50 μM		DMSO	Has no Effect on forskolin-induced cAMP signaling in human HEK293T cells coexpressing CRE	22260203
IEC-6	Function Assay		6 h		Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced axin2 expression with IC50 of 0.64 μM	24060489
IEC-6	Function Assay		6 h		Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced lgr5 expression with IC50 of 2.9 μM	24060489
DLD1	Function Assay	20 μM	24 h	DMSO	Inhibition of tankyrase assessed as inhibition of TCF-dependent transcriptional activity	24527792
DLD1	Cytotoxic Assay	20 μM	10 d	DMSO	Cytotoxicity assessed as growth inhibition	24527792
VERO	Function Assay	25 μM		DMSO	Disturbes PAR belt synthesis, affecting the actin cytoskeleton, cell shape and cell adhesion	25332845
HeLa	Function Assay	10 μM	48 h		Reduction of cytoplasmic distribution and nuclear translocation of β-catenin	25061499
SiHa	Function Assay	10 μM	48 h		Reduction of cytoplasmic distribution and nuclear translocation of β-catenin	25061499
HEK293	Function assay				Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin, IC50 = 0.078 μM.	23844574
DLD1	Function assay		24 hrs		Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay, IC50 = 0.707 μM.	25299683
Sf21	Function assay		2 hrs		Inhibition of N-terminal GST-tagged human TNKS-2 (849 to 1166 residues) expressed in in insect sf21 cells preincubated for 2 hrs followed by substrate addition measured after 30 mins, IC50 = 0.017 μM.	27163581
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
A549	Growth inhibition assay		72 hrs		Growth inhibition of human A549 cells after 72 hrs by MTT assay, IC50 = 12.3 μM.	29934219
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 12 mg/mL (38.42 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.
Clear solution	4%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (3.20mM)	Taking the 1 mL working solution as an example, add 40 μL of 25 mg/ml clear DMSO stock solution to 960 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.
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.
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.
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.

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:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% 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.

Chemical Information, Storage & Stability

Molecular Weight	312.31	Formula	C₁₄H₁₁F₃N₂OS	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	284028-89-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NVP-XAV939			Smiles	C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F

Mechanism of Action

Targets/IC₅₀/Ki	TNKS2 (Cell-free assay) 4 nM TNKS1 (Cell-free assay) 11 nM
In vitro	XAV-939 specifically inhibits tankyrase PARP activity. This compound 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 exposure. Treatment of human lymphoblasts with 1.0 μM this chemical results in marked elevation of tankyrase 1 levels. This agent is axin stabilizing agent. It stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. This compound 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. This chemical deregulates the Wnt/b-catenin pathway which has been implicated in many cancers.
In vivo	XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21037379/ [2] https://pubmed.ncbi.nlm.nih.gov/19759537/ [3] https://pubmed.ncbi.nlm.nih.gov/33128175/

Applications

Methods	Biomarkers	Images	PMID
Western blot	β-catenin / E-cadherin / N-cadherin β-catenin / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin		31060551
Immunofluorescence	β-catenin / E-cadherin Actin / PAR Hes1 / β-catenin / p-STAT3		31060551

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

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

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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

XAV-939 WNT Pathway Inhibitor

Chemical Structure

Molecular Weight: 312.31