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.
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
NVP-TNKS656
Dangerous GoodsCAS number：1419949-20-4 molecular formula：C27H34N4O5
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 1-Piperidineacetamide,N-(cyclopropylmethyl)-4-(4-methoxybenzoyl)-N-[(3,5,7,8-tetrahydro-4-oxo-4H-pyrano[4,3-d]pyrimidin-2-yl)methyl]- | ||
| CAS number | 1419949-20-4 | molecular formula | C27H34N4O5 |
| molecular weight | 494.58 g/mol | Exact mass | - |
| PSA | 101.000 Ų | logp | 1.014 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P273: 避免释放到环境中。 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P391: 收集溢出物 P330: 漱口 P301+P312: 如误吞咽：如感觉不适，呼叫急救中心/医生。
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
