中文名：NVP-TNKS656
英文名：NVP-TNKS656
纯度：Moligand™，≥99%
货号：N413722
Cas号：1419949-20-4
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
NVP-TNKS656 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.
Targets
TNKS2 (Cell-free assay) 6 nM
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.
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关键字： 1-?Piperidineacetamide,N-?(cyclopropylmethyl)?-?4-?(4-?methoxybenzoyl)?-?N-?[(3,?5,?7,?8-?tetrahydro-?4-?oxo-?4H-?pyrano[4,?3-?d]?pyrimidin-?2-?yl)?methyl]?-
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