|Solubility:||DMSO up to 100 mM; EtOH up to 100 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
NVP-TNKS656 is a highly potent, selective and oral bioavailable tankyrase inhibitor with IC50 of 6 nM for TNKS2. It has 300-fold selectivity against PARP1 and PARP2. In MMTV-Wnt1 tumor models, NVP-TNKS656 was dosed to mice orally to stabilize Axin1 protein and reduce the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth.
How to Use:
In vitro: NVP-TNKS656 was used at 10 µM in vitro and cellular assays.
In vivo: In MMTV-Wnt1 tumor bearing athymic nude mice, NVP-TNKS656 was dosed to mice orally at 100-350 mg/Kg once per day to stabilize Axin1 protein and reduce the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth.
- 1. Shultz MD, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor. (2013) J Med Chem. 56(16):6495-511.
- 2. Arqués O, et al. Tankyrase Inhibition Blocks Wnt/β-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer. (2016) Clin Cancer Res. 22(3):644-56.
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