| Description | 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. |
| In vitro | XMD16-5在抑制TNK2磷酸化方面表现出强效。XMD8-87与XMD16-5能强力抑制在实体瘤类型中发现的TNK2截断突变的磷酸化。 |
| Cell experiments | 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) |
| Target activity | R806Q:77 nM, D163E:16nM |
| molecular weight | 416.48 |
| Molecular formula | C23H24N6O2 |
| CAS | 1345098-78-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (108.05 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 5 mg/mL (12.01 mM) |
| References | 1. Maxson JE, et al. Cancer Res. 2016, 76(1):127-38. |