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（ 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，请先与我们客服联系。| 中文名称: | XAV939 促销 一键复制产品信息 | ||||
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| 英文名称: | XAV939 | ||||
| 别名: | 3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one | ||||
| CAS No: | 284028-89-3 | 分子式: | C14H11F3N2Os | 分子量: | 312.31 |
| CAS No: | 284028-89-3 | ||||
| 分子式: | C14H11F3N2Os | ||||
| 分子量: | 312.31 | ||||
| MDL: | MFCD16879017 | ||||
熔点：
207.14°C
包装规格：
5mg 25mg 100mg in glass bottle
溶解性：
溶于PBS (pH 7.2) 、(~0.15 mg/ml)、DMSO (~2 mg/ml)、DMF (~5 mg/ml)、水(<1 mg/ml at 25°C）和乙醇 (<1 mg/ml at 25 °C）.
产品描述：
基本信息
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产品编号：X10005 |
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产品名称：XAV939 |
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CAS: |
284028-89-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
312.31 |
-20℃ |
一个月 |
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化学名： |
3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one |
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Solubility (25°C) |
体外 |
DMSO |
12mg/mL (38.42mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内（现配现用） |
4% DMSO+corn oil |
1mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.2019mL |
16.0097mL |
32.0195mL |
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5mM |
0.6404mL |
3.2019mL |
6.4039mL |
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10mM |
0.3202mL |
1.6010mL |
3.2019mL |
生物活性
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产品描述 |
有效的 tankyrase 抑制剂，靶向 Wnt/β-catenin 途径。 |
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靶点/IC50 |
TNKS2 4nM |
TNKS1 11nM |
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体外研究 |
XAV939 also binds to recombinant PARP1, although with a significantly lower binding affinity (Kd=1.2μM). XAV939 (1μM) strongly inhibis STF activity in SW480 cells, Wnt3a-stimulated STF activity in HEK293 cells, but does not affect CRE, NF-κB or TGF-β luciferase reporters. XAV939 regulates axin levels through tankyrase inhibition in HEK293 cell[1]. XAV939 (0.5μM, 1.0μM) reduces DNA-PKcs protein levels 50% of the relative DMSO control in human lymphoblasts. XAV939 induces a second wave of pro-cardiomyocyte gene expression as shown by increased Mesp1 and Isl1expression 2 to 4 days after Wnt inhibition, and by increased Nkx2.5 expression 4 to 6 days after XAV939 addition. XAV-939 (10nM) has a suppressive effect on elevated MMP-13 levels in both IL-1β-induced SW 1353 cells. |
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体内研究 |
XAV-939 (3mL, 10nM) has a suppressive effect on elevated MMP-13 levels in the rat OA model. XAV-939 (1mg/mL, i.p.) ameliorates the psoriasiform skin disease induced by IMQ. XAV-939 results in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice. |
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推荐实验方法(仅供参考)
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激酶实验： |
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Kinase Assay |
To assess the effect of compounds on auto-PARsylation of TNKS, 1μM GST fusion protein containing the SAM domain and the PARP domain of TNKS2 (a.a. 872-1166) is mixed with 5μM biotin-NAD+ and 2μM XAV939 or LDW643 at 30°C for 2.5 hours.Samples are resolved by SDS-PAGE and probed with streptavidin AlexaFluor680. To assess PARsylation of axin, recombinant full-length TNKS2 (expressed/purified as a N-terminal His-tagged protein in bacteria) is incubated with GST-axin 1 (1-280) in the presence of biotin-NAD+ with or without XAV939. The products are resolved and probed with Streptavidin-HRP and imaged using a AlphaInnotech imager. To assess the effect of XAV939, IWR-1-enod, IWR-1-exo, and ABT-888 on autoPARsylation of TNKS2, His-tagged full-length TNKS2 is incubated with 5μM biotin-NAD+ and 3mM of indicated compounds.The products are resolved and probed with Streptavidin-HRP. LC/MS-based high throughput auto-PARsylation assays for PARP1, PARP2, TNKS1, and TNKS2 are setup to monitor the formation of nicotinamide (a by-product of the PARsylation reaction) in the presence of small molecule inhibitors. |
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细胞实验: |
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Cell Assay |
Human SW 1353 chondrosarcoma cells are seeded in 96-well plates (1×104 cells/well) and are treated with Icariin (0, 5, 10, 20, 40, 80, or 100μM). After 24 h, 20μL MTT (5mg/mL in PBS) is added to each well and plates are incubated at 37°C for another 4h. Supernatants are then removed, and 150μL DMSO is added to each well. After plates are shaken for 10 min,optical density values measured at 570nm are recorded using an ELISA reader. |
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动物实验: |
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Animal Administration |
C57BL/6J mice are kept under specific pathogen-free conditions. XAV-939 is injected i.p., at a dose of 1mg/mL, once a day for seven consecutive days of IMQ treatment (injection volume 100μL). Control mice are injected with 100μL 10% DMSO/90% 0.9% NaCl, the solvent for XAV-939. To ameliorate any suffering of mice observed throughout these experimental studies, they are euthanized by CO2 inhalation. |
保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
(2).jpg)
体内配方的制备方法: 取 50μLDMSO 母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清
方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
以上为“动物实验计算换算器”的使用方法举例，并不是具体某个试剂的配制，请根据您的实验动物和给药方式选择适当的溶解方案。
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL Saline/PBS/ddH2O，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
