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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $39 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $126 | In Stock | |
25 mg | $283 | In Stock | |
50 mg | $455 | In Stock | |
100 mg | $672 | In Stock | |
500 mg | $1,430 | In Stock | |
1 mL x 10 mM (in DMSO) | $79 | In Stock |
Description | 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. |
Targets&IC50 | D163E mutations:16nM, R806Q mutations:77 nM |
In vitro | 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. |
Kinase Assay | 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]. |
Cell Research | 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) |
Alias | ACK1-B19 |
Molecular Weight | 445.52 |
Formula | C24H27N7O2 |
Cas No. | 1234480-46-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 5.33 mg/mL (11.97 mM), Sonication is recommended. ![]() H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 5 mg/mL (11.2 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
Ethanol/DMSO
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