Source | M.W. | 312.31 | CAS No. | 284028-89-3 | |
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Structural Info | |||||
Formulation | Powder | ||||
Reconstitution | Before reconstitution, we recommend a brief spin todrive down any material dislodged from the bottom of the tube. The compound is soluble in DMSO. | ||||
Stability | The powder is stable for at least 2 year if stored at-20 °C.The dissolved compound isstable for at least 1 month at 4 °C, but should be stored in aliquots at-20 °C for longer term. Protectfrom light. | ||||
Purity | Greater than 98% as determined by LC/MS analysis.LC/MS and/or NMR data available upon request. | ||||
Biological Activity | In a cell-based assay measuring the activation of the TCF reporter gene, this compound gives IC50 of 300 nM. | ||||
Country of Origin |
XAV-939,2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-one,is an inhibitor of Tankryases with IC50 of 11 and 4nM for Tankyrase 1 andTankyrase 2, respectively. It stimulatesβ-catenin degradation by stabilizing axin, resulting in the inhibition ofthe canonical WNT pathway. Bothtankyrase isoforms interact with a highly conserved domain of axin andstimulate its degradation through the ubiquitin-proteasome pathway. Tankryaseinhibitors are potential therapeutics for cancers as deregulated Wnt/β-cateninpathway activity has been implicated in many cancers.Ref: Huang SM et al. Nature. 2009 Oct 1;461(7264):614-20.