Biological Activity
Potent Ack1/TNK2 inhibitor (IC50 = 38 and 113 nM in Ba/F3 cell lines containing leukemia-associated D163E and R806Q mutations respectively). Blocks phosphorylation of TNK2 receptors containing solid-tumor type truncation mutations.
Licensing Information
Sold under license from Dana-Farber Cancer Institute.
Technical Data
| M. Wt | 445.52 |
| Formula | C24H27N7O2 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1234480-46-6 |
| PubChem ID | 53322923 |
| InChI Key | LGLHCXISMKHLIK-UHFFFAOYSA-N |
| Smiles | COC1=C(C=CC(N2CCN(CC2)C)=C1)NC3=NC=C4NC(C5=CC=CC=C5N(C4=N3)C)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 44.55 | 100 | |
| DMSO | 22.28 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 445.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.24 mL | 11.22 mL | 22.45 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.49 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
Maxson et al (2015) Identification and characterization of tyrosine kinase nonreceptor 2 mutations in leukemia through integration of kinase inhibitor screening and genomic analysis. Cancer.Res. 76 127 PMID: 26677978
Maxson et al (2014) Development and repurposing of small-molecule kinase inhibitors to target novel leukemogenic TNK2 mutations Blood 124 435 PMID:
Keywords: XMD 8-87, supplier, XMD8-87, Inhibitors, inhibits, Ack1, TNK2, Ba/F3, leukemia, D163E, R806Q, phosphorylation, tyrosine, kinase, 2, Ack1, Tocris Bioscience
