产品信息
商品描述
NVP-TNKS656 is a highly potent, selective, and orally active <b>tankyrase</b> inhibitor with <b>IC50</b> of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
分子量
494.58
纯度
99.85 %
可溶性
体外:
DMSO 100mg/mL(202.19mM)
Ethanol 10mg/mLwarming(20.21mM)
Water <1mg/mL
DMSO 100mg/mL(202.19mM)
Ethanol 10mg/mLwarming(20.21mM)
Water <1mg/mL
In vitro(体外研究)
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(体内研究)
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.
背景
分子式
C27H34N4O5
CAS号
1419949-20-4
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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