Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XAV-939 (NVP-XAV939) 是一种 Tankyrase (TNKS) 抑制剂,抑制 TNKS1 和 TNKS2 (IC50=11/4 nM)。XAV-939 可以选择性抑制 Wnt/β-catenin 介导的转录。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 348 | 现货 | ||
10 mg | ¥ 467 | 现货 | ||
25 mg | ¥ 868 | 现货 | ||
50 mg | ¥ 1,567 | 现货 | ||
100 mg | ¥ 2,353 | 现货 | ||
200 mg | ¥ 2,970 | 现货 | ||
500 mg | ¥ 4,910 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 364 | 现货 |
产品描述 | XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription. |
靶点活性 | TNKS1:11 nM (cell free), TNKS2:4 nM (cell free) |
体外活性 |
方法:人结直肠癌细胞 SW480 用 XAV-939 (1 µM) 处理 16 h,使用 Western Blot 检测靶点蛋白表达水平。 结果:XAV-939 降低 SW480 细胞中 β-catenin 的丰度并增加 axin 和 p-β-catenin 的丰度。[1] 方法:正常人表皮角质形成细胞 NHEK 用 XAV-939 (10-50 µM) 和 rhIL-6 (50 ng/mL) 处理 24 h,使用 APC BrdU flow kit 检测靶细胞数。 结果:XAV-939 基本上抑制了 NHEK 的过度增殖。[2] |
体内活性 |
方法:为研究 Wnt 信号的体内功能,将 XAV-939 (1 mg/mL,100 μL,10% DMSO/90% 0.9% NaCl) 腹腔注射给 IMQ 诱导的银屑病小鼠模型,每天一次,持续七天。 结果:XAV-939 的给药导致小鼠 IMQ 诱导的表皮增生和真皮炎症浸润显著减少。XAV-939 给药显著减少了 IMQ 诱导的炎症皮肤病变中 F4/80+ 巨噬细胞和 CD3+T 细胞的浸润。Wnt 信号传导对 IMQ 介导的表皮增生至关重要。[2] 方法:为检测体内抗肿瘤活性,将 paclitaxel (10 mg/kg) 和 XAV-939 (10 mg/kg) 腹腔注射给携带人乳腺癌肿瘤 MDA-MB-231 的 BALB/c nude 鼠,每周两次,持续四周。 结果:与对照和每种单一治疗相比,paclitaxel 和 XAV-939 的联合治疗可以有效抑制乳腺肿瘤的生长。[3] |
细胞实验 | XAV939, the recently identified small molecule shown to specifically inhibit PARP activity of tankyrase 1 (and tankyrase 2 at higher concentrations), was used here at much lower concentrations than 3-AB. The tankyrase specific inhibitor XAV939 was solubilized in DMSO at 55°C to a stock concentration of 10mM, which was diluted to a working concentration of 100μM; final concentrations of 0.5μM or 1μM were well within the concentration parameters suggested for cell culture experiments to inhibit tankyrase specifically. Cultures were maintained under these conditions for the duration of the designated time course. Controls were exposed to DMSO alone. Following treatment, cells were lysed and prepared for western blot analysis. Tankyrase 1 and DNA-PKcs protein levels were normalized to the β-actin loading controls and quantified [1]. |
动物实验 | XAV-939, a selective inhibitor of tankyrase (TNKS)-1 and TNKS-2, was injected i.p., at a dose of 1 mg/ml, once a day for seven consecutive days of IMQ treatment (injection volume 100 μl). Control mice were injected with 100 μl 10% DMSO/90% 0.9% NaCl, the solvent for XAV-939 [3]. |
别名 | XAV939, NVP-XAV939 |
分子量 | 312.31 |
分子式 | C14H11F3N2OS |
CAS No. | 284028-89-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12.5 mg/mL (40.02 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2019 mL | 16.0097 mL | 32.0195 mL | 80.0487 mL |
5 mM | 0.6404 mL | 3.2019 mL | 6.4039 mL | 16.0097 mL | |
10 mM | 0.3202 mL | 1.601 mL | 3.2019 mL | 8.0049 mL | |
20 mM | 0.1601 mL | 0.8005 mL | 1.601 mL | 4.0024 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
XAV-939 284028-89-3 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Stem Cells PARP Wnt/beta-catenin poly ADP ribose polymerase XAV939 Inhibitor XAV 939 NVP-XAV-939 NVP-XAV939 β-catenin NVP-XAV 939 inhibit Beta catenin inhibitor