Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XMD16-5 是TNK2抑制剂,对D163E 和R806Q 突变体的IC50值分别为16和77nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 363 | 现货 | ||
2 mg | ¥ 532 | 现货 | ||
5 mg | ¥ 877 | 现货 | ||
10 mg | ¥ 1,450 | 现货 | ||
25 mg | ¥ 2,350 | 现货 | ||
50 mg | ¥ 3,480 | 现货 | ||
100 mg | ¥ 4,970 | 现货 | ||
500 mg | ¥ 10,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 983 | 现货 |
产品描述 | XMD16-5 is a TNK2 inhibitor. TNK2 genomic amplification has been associated with late-stage or metastatic lung and prostate Ys. Overexpression of TNK2 promoted metastasis in a mouse model of breast Y. TNK2 signaling is disrupted in breast, prostate and gastrointestinal tumors. |
靶点活性 | R806Q:77 nM, D163E:16nM |
体外活性 | XMD16-5 is found to be potent in the inhibition of TNK2 phosphorylation. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types. |
激酶实验 | Kinase targets are tested with biochemical enzymatic kinase assays using the SelectScreen Kinase Profiling Service to determine IC50 values. The compounds (XMD16-5) are assayed at 10 concentrations (3-fold serial dilutions starting from 1 μM) at an ATP concentration equal to the ATP Km[1]. |
细胞实验 | 293T cells expressing TNK2 are plated in 6-well format at a density of 250,000 cells per well 48 hours prior to treatment. Cells are then treated with a 100 μL of XMD8-87 or XMD16-5 at 5 μmol/L and with 9 1:1 serial dilutions down to ≈10 nmol/L. Two additional samples are treated with DMSO only. Cells are then incubated for 6 hours at 37°C. Protein extraction is accomplished by adding 300 μL of lysis buffer to cells after removing media. Plates are gently shaken for 5 minutes at room temperature. Lysates are collected and cleared of incompletely solubilized material by spinning for 10 minutes at maximum speed in a microcentrifuge. Samples are prepared for SDS-PAGE using the EPage loading buffer.(Only for Reference) |
分子量 | 416.48 |
分子式 | C23H24N6O2 |
CAS No. | 1345098-78-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 77 mg/mL (185 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 5 mg/mL (12.01 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.4011 mL | 12.0054 mL | 24.0108 mL | 60.0269 mL |
5 mM | 0.4802 mL | 2.4011 mL | 4.8022 mL | 12.0054 mL | |
10 mM | 0.2401 mL | 1.2005 mL | 2.4011 mL | 6.0027 mL | |
DMSO | 20 mM | 0.1201 mL | 0.6003 mL | 1.2005 mL | 3.0013 mL |
50 mM | 0.048 mL | 0.2401 mL | 0.4802 mL | 1.2005 mL | |
100 mM | 0.024 mL | 0.1201 mL | 0.2401 mL | 0.6003 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。
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