Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 3,5,7,8-tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
Purity: ≥98%
Formula Markup: C14H11F3N2OS
Formula Weight: 312.3
CAS Number: 284028-89-3
Notes: The Wnt signaling pathway is integral to normal biological processes and inappropriately active in many cancers. It is regulated through degradation of the downstream effector β-catenin via a complex consisting of the tumor suppressor APC, axin, and glycogen synthase kinase 3 (GSK3). Axin is the concentration-limiting factor for this degradation complex. Initially indentified as telomere-associated proteins{6770}, tankyrases promote axin ubiquitination, possibly through poly-ADP-ribosylation (PARsylation).{17502} XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively.{17502} By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells.{17502} At concentrations as low as 0.33 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.{17502}
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