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.
Neural Plast. 2021 Apr 19;2021:6680192.
The Wnt/ β-Catenin Pathway Regulated Cytokines for Pathological Neuropathic Pain in Chronic Compression of Dorsal Root Ganglion Model
XAV939 purchased from AbMole
Cell Communication & Signaling. 2020 Sep 10.
JARID1B promotes colorectal cancer proliferation and Wnt/β-catenin signaling via decreasing CDX2 level
XAV939 purchased from AbMole
Pharmacol Res. 2020 Jul;157:104831.
Astragaloside IV acts through multi-scale mechanisms to effectively reduce diabetic nephropathy
XAV939 purchased from AbMole
EBioMedicine. 2020 Jan 14.
Systematic Investigation on Multi-Scale Mechanisms of Astragaloside IV in Treating Diabetic Nephropathy
XAV939 purchased from AbMole
Stem Cell Res. 2020 Mar;43:101698.
Cryopreservation of human pluripotent stem cell-derived cardiomyocytes is not detrimental to their molecular and functional properties.
XAV939 purchased from AbMole
Eur Rev Med Pharmacol Sci. 2017 Apr;21(8):1980-1989.
Isoflurane and sevoflurane affects Wnt/β-catenin signaling pathways in hippocampal formation of neonatal rats
XAV939 purchased from AbMole
Cell Experiment | |
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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 | |
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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 |
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
Molecular Weight | 312.3 |
Formula | C14H11F3N2OS |
CAS Number | 284028-89-3 |
Purity | 98.79% |
Solubility | DMSO 11 mg/mL |
Storage | at -20°C |
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