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.

99.85 %

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

体外:
DMSO 100mg/mL(202.19mM)
Ethanol 10mg/mLwarming(20.21mM)
Water <1mg>

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 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.

[1] Shultz MD, et al. J Med Chem. 2013, 56(16), 6495-6511.

[2] Arqués O, et al. Clin Cancer Res. 2016, 22(3), 644-656.