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XAV939 (CAS 284028-89-3)

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Solicitud:A potent inhibitor of beta-catenin, tankyrase 1, and tankyrase 2
Número CAS:284028-89-3
Pureza:≥98%
Peso Molecular:312.3
Fórmula Molecular:C14H11F3N2OS
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Nombre del productoNúmero de catálogoUnidadPrecioCantidadAñadir 
XAV939 sc-296704 1 mg $25
XAV939 sc-296704A 5 mg $51
XAV939 sc-296704B 50 mg $625
Descripción
XAV939 is a potent, small molecule inhibitor of tankyrase (TNKS) 1 and 2 with IC50 values of 11 and 4 nM, respectively. 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 beta-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 proteins1, tankyrases promote axin ubiquitination, possibly through poly-ADP-ribosylation (PARsylation). By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of beta-catenin in SW480 cells. At concentrations as low as 0.3 µM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.
Información Técnica
Apariencia:A crystalline solid
Estado Físico:Solid
Solubilidad:Soluble in 1:5 EtOH:PBS (pH 7.2) (~0.15 mg/ml), DMSO (~2 mg/ml), DMF (~5 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C.
Almacenamiento:Store at -20° C
Punto de Ebullición:429.31 °C at 760 mmHg (Predicted)
Densidad:~1.42 g/cm3 (Predicted)
Índice de Refracción:n20D 1.63 (Predicted)
IC50:Tankyrase 1: IC50 = 11 nM; Tankyrase 2: IC50 = 4 nM; Protein Wnt-3a: IC50 = 51 nM (human); Catenin beta-1: IC50 = 51 nM (human)
Seguridad e Información de Referencia
WGK Alemania:3
Número MDL:MFCD00004437
Número EC:206-765-9
SMILES:O=C(NC1=CC=C(C(NO)=O)C=C1)[C@@H]([C@H](C)C)C2=CC=CC=C2
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
References
1 Smith, S., Giriat, I., Schmitt, A., et al. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science 282, 1484-1487 (1998 Nov). 2 Huang, S.A., Mishina, Y.M., Liu, S., et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature 461 614-619 (2009).
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