化合物XMD8-87 T3709

Product Introduction
Bioactivity


英文名: XMD8-87

描述: 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。

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)

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].

体外活性: XMD8-87 在抑制TNK2磷酸化方面显示出高效能。XMD8-87 和 XMD16-5 强效抑制在实体肿瘤类型中发现的TNK2截断突变的磷酸化。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 65 mg/mL (145.89 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 5 mg/mL(11.2 mM)


关键字: Tyrosinase | XMD8-87 | Inhibitor | inhibit | XMD8 87 | XMD-8-87 | XMD887

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