NVP-TNKS656
产品说明书
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同义名 : | TNKS656 |
| CAS号 : | 1419949-20-4 | |
| 货号 : | A474769 | |
| 分子式 : | C27H34N4O5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 494.58 | |
| MDL号 : | MFCD28167762 | |
| 存储条件： |
Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Tankyrase 1 and 2 have been shown to be redundant, druggable nodes in the Wnt pathway. NVP-TNKS656 is a novel and selective tankyrase 2 inhibitor with IC50 value of 6nM, while exhibits inhibitory effect on PARP 1 and 2 with IC50 values up to >19μM and 32μM, respectively. NVP-TNKS656 exhibited a good PK/PD relationship as a corresponding 70−80% reduction in the Wnt/beta-catenin target gene Axin2 mRNA level, compared to vehicle control animals, could be observed in MMTV-Wnt1 tumor bearing athymic nude mice after a single oral dose of NVP-TNKS656 at 350 mg/kg over a 24-h time. Inhibition of Tankyrases through NVP-TNKS656 could potentiate MEK inhibitor activity by releasing a FGFR2 signaling feedback loop, as well as synergize with MEK inhibitor to downregulate FGFR2 signaling and enhance antitumor activity in vivo. Intraperitoneal injection with 100mg/kg twice daily blocked the Wnt/β-catenin signaling in colorectal cancer PDX models shown by reduction of nuclear β-catenin and increase of AXIN1 protein levels. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.02mL 0.40mL 0.20mL |
10.11mL 2.02mL 1.01mL |
20.22mL 4.04mL 2.02mL |
| 参考文献 |
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