Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XMD8-87 (ACK1-B19)是TNK2抑制剂,对于D163E 和R806Q 突变体的IC50值分别为38和113 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 289 | 现货 | ||
2 mg | ¥ 423 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,280 | 现货 | ||
25 mg | ¥ 2,870 | 现货 | ||
50 mg | ¥ 4,280 | 现货 | ||
100 mg | ¥ 6,130 | 现货 | ||
500 mg | ¥ 12,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | XMD8-87 (ACK1-B19) is a TNK2 inhibitor with activity in the inhibition of TNK2 phosphorylation. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types. |
靶点活性 | D163E mutations:16nM, R806Q mutations:77 nM |
体外活性 | XMD8-87 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 (XMD8-87) 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) |
别名 | ACK1-B19 |
分子量 | 445.52 |
分子式 | C24H27N7O2 |
CAS No. | 1234480-46-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 65 mg/mL (145.89 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 5 mg/mL(11.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.2446 mL | 11.2228 mL | 22.4457 mL | 56.1142 mL |
5 mM | 0.4489 mL | 2.2446 mL | 4.4891 mL | 11.2228 mL | |
10 mM | 0.2245 mL | 1.1223 mL | 2.2446 mL | 5.6114 mL | |
DMSO | 20 mM | 0.1122 mL | 0.5611 mL | 1.1223 mL | 2.8057 mL |
50 mM | 0.0449 mL | 0.2245 mL | 0.4489 mL | 1.1223 mL | |
100 mM | 0.0224 mL | 0.1122 mL | 0.2245 mL | 0.5611 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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