Molecular Weight(MW): 494.58
NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
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|Description||NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.|
In vitro, NVP-TNKS656 shows low to moderate microsomal ER values across species and high solubility.  In PI3K or AKT inhibitor-resistant cells, NVP-TNKS656 blocks Wnt/β-Catenin pathway and promotes apoptosis. 
|In vivo||In mice, NVP-TNKS656 displays low clearance and volume of distribution, and exhibits good exposure and moderate oral bioavailability. In MMTV-Wnt1 tumor bearing athymic nude mice, NVP-TNKS656 (350 mg/kg, p.o.) stabilizes Axin1 protein and reduces 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. |
|In vitro||DMSO||100 mg/mL (202.19 mM)|
|Ethanol||10 mg/mL warmed (20.21 mM)|
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