NVP-TNKS656 是一种可口服的选择性TNKS2抑制剂，IC50值为 6 nM。

NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor.

In vitro, NVP-TNKS656 shows low to moderate microsomal ER values across species and high solubility. [1] In PI3K or AKT inhibitor-resistant cells, NVP-TNKS656 blocks Wnt/β-Catenin pathway and promotes apoptosis. [2]

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%. [1] In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth. [2]

1419949-20-4

C27H34N4O5

494.592

TNKS656

H2O:<1 mgml
Ethanol:10 mg/mL(20.21 mM),warming
DMSO:93 mg/mL (188 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years