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XAV939

Cat. No. M1796
XAV939 Structure
Synonym:

XAV-939

Size Price Availability Quantity
25mg USD 100 In stock
50mg USD 185 In stock
100mg USD 280 In stock
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Quality Control
Biological Activity

XAV939 is an inhibitor of Tankryases with IC50 values of 11 and 4nM for Tankyrase 1 and Tankyrase 2, respectively. It stimulates beta-catenin degradation by stabilizing axin, resulting in the inhibition of the canonical Wnt pathway. Wnt proteins act on a variety of stem cells that include neural, mammary and embryonic stem cells. XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells. In addition, XAV939 inhibits growth of DLD-1 cells, an APC-deficient colorectal cancer cell line.

Protocol
Cell Experiment
Cell lines B-T549, MDA-MB-231, HCC-1143 and HCC-1937 cell lines
Preparation method Cell viability assay. Cells were seeded at 20,000 cells/well into 96-well plates. After overnight incubation, cells were treated with DMSO or each Wnt inhibitor (iCRT-3, 75 μM; iCRT-5, 200 μM; iCRT-14, 50 μM; IWP-4, 5 μM and XAV-939, 10 μM) for 48 hours. Cell viability was determined using the Cell Titer-Glo luminescent cell viability assay kit (Promega) according to the manufacturer’s instructions. Luminescence was measured using FLUOstar microplate reader. All treatments were performed in triplicate, and each experiment was repeated three times.
Concentrations 10 μM
Incubation time 48 hr
Animal Experiment
Animal models bleomycin-induced dermal fibcrosis mice model
Formulation 10% DMSO / 90% normal saline
Dosages 2.5 mg/kg, four times a day
Administration Intraperitoneal injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 312.3
Formula C14H11F3N2OS
CAS Number 284028-89-3
Purity 100.00%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Eur Med Pharmacol Sci (2017). XVA 939, Figure 4. (AbMole BioScience, Shanghai, China)
Method
Cell Lines
Concentrations 2 mg/ml
Incubation Time 30 min
Results Wnt inhibitor XAV 939 was significantly inhibited the up-regulation of Wnt and phosphorylated-β-catenin and increased phosphorylated-GSK-3β expression in the hippocampus in ISA and SEA groups, as compared with the control group at 5 weeks (Figure 4 A, B, C, p < 0.05).
Rating
Source Eur Med Pharmacol Sci (2017). XVA 939, Figure 3. (AbMole BioScience, Shanghai, China)
Method
Cell Lines
Concentrations 2 mg/ml
Incubation Time 30 min
Results As shown in Figure 3, the expression levels of Wnt3a and β-catenin (Figure 3A, C, p < 0.05) were significantly reduced after Wnt inhibitor XAV 939 treatment, while GSK-3β expression level was dramatically increased in ISAI and SEAI groups (Figure 3B, p < 0.05).
Rating
Source Eur Med Pharmacol Sci (2017). XVA 939, Figure 2. (AbMole BioScience, Shanghai, China)
Method
Cell Lines
Concentrations 2 mg/ml
Incubation Time 30 min
Results P7 rats treated with Wnt inhibitor XAV 939 could markedly relief that damage. Those morphological changes were significantly moderated and reduced neuronal loss at 10-week (Figure 2).
Rating
Source Eur Med Pharmacol Sci (2017). XVA 939, Figure 1. (AbMole BioScience, Shanghai, China)
Method
Cell Lines
Concentrations 2 mg/ml
Incubation Time 30 min
Results When rats were treated with Wnt inhibitor XAV 939 at 30 min before anesthesia, the impairment of brain could relieve. These findings suggested that impairment of learning and memory in P7 rats may through the Wnt signaling pathway.
Rating
Product Citations
References

Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells.
Bilir B, et al. J Transl Med. 2013 Nov 4;11:280. PMID: 24188694.

Inactivation of tankyrases reduces experimental fibrosis by inhibiting canonical Wnt signalling.
Distler A, et al. Ann Rheum Dis. 2013 Sep 1;72(9):1575-80. PMID: 23148305.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: XAV939, XAV-939 supplier, Wnt/beta-catenin, inhibitors

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