| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 南京 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S86830-5mg |
≥99%(HPLC) | ￥570.00 |
10 | - | - | - | - |
|
S86830-10mg |
≥99%(HPLC) | ￥830.00 |
8 | - | - | - | - |
|
S86830-25mg |
≥99%(HPLC) | ￥1800.00 |
4 | - | - | - | - |
|
S86830-50mg |
≥99%(HPLC) | ￥3100.00 |
4 | - | - | - | - |
|
S86830-100mg |
≥99%(HPLC) | ￥5230.00 |
3 | - | - | - | - |
|
| 产品描述： | JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM. | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | IC50: 420 nM (Wnt);Wnt/beta-catenin | ||||||||||||||||||||
| 体外研究： | JW74 shows a reduction of canonical Wnt signaling in the ST-Luc assay with an IC50 of 790 nM. The effect of tankyrase inhibition on cellular viability is tested by performing an MTS assay. The cellular viability of U2OS cells treated for 72 h treatment with 10 μM JW74 is reduced to 80%, relative to DMSO-treated cells. Flow cytometry is also performed to determine the expression marker Ki-67 in U2OS following 48 h treatment with DMSO or 10 uM JW74. Ki-67 expression is reduced from 97.5% in DMSO-treated cells to 86.7% in JW74-treated cells | ||||||||||||||||||||
| 体内研究： | The in vivo efficacy of JW74 is tested using SW480 cell xenografts. A relatively high dose of JW74 (150 or 300 mg/kg) is used because of a rapid compound degradation in the organism as indicated in the human liver microsome analysis (t1/2=2.5 minutes) and in pharmacokinetic analyses (after per oral injections: t1/2=30 minutes and intravenous injections: t1/2=15 minutes). The presence of JW74 in tumors and plasma is identified by mass spectrometry. JW74 concentration in tumors is in the range 4.2 to 72.1 μmol/kg for JW74 150 mg/kg, 1.9 to 11.1 μmol/kg for JW74 300 mg/kg, and 2.8 μM in plasma for both doses | ||||||||||||||||||||
| 参考文献： | 1. Waaler J, et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205. 2. Stratford EW, et al. The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. Cancer Med. 2014 Feb;3(1):36-46. | ||||||||||||||||||||
| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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北京