Biological Activity
Potent and selective haspin kinase inhibitor (IC50 = 2 nM). Selective over 27 other protein kinases including Aurora B kinase. Induces cell cycle arrest at G2/M, inhibits cell proliferation and promotes apoptosis in multiple cancer cell lines. Inhibits angiogenesis ex vivo and attenuates tumor growth of HCT-116 xenografts in rats.
Compound Libraries
CHR 6494 trifluoroacetate is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 406.36 |
| Formula | C16H16N6.CF3CO2H |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1458630-17-5 |
| PubChem ID | 91691123 |
| InChI Key | ILWYDZNXJQESDI-UHFFFAOYSA-N |
| Smiles | CCCNC2=NN1C(C3=CC(C=NN4)=C4C=C3)=CN=C1C=C2.OC(C(F)(F)F)=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 | |||
| DMSO | 40.64 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 406.36. 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 | 2.46 mL | 12.3 mL | 24.61 mL |
| 5 mM | 0.49 mL | 2.46 mL | 4.92 mL |
| 10 mM | 0.25 mL | 1.23 mL | 2.46 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Huertas et al (2012) Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene 31 1408 PMID: 21804608
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