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Submit ReviewCHR 6494 trifluoroacetate
Description: Potent and selective haspin inhibitor
Chemical Name: 3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine trifluoroacetate
Purity: ≥98% (HPLC)
Biological Activity for CHR 6494 trifluoroacetate
CHR 6494 trifluoroacetate is a 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 for CHR 6494 trifluoroacetate
CHR 6494 trifluoroacetate is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for CHR 6494 trifluoroacetate
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CHR 6494 trifluoroacetate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.64 | 100 |
Preparing Stock Solutions for CHR 6494 trifluoroacetate
The following data is based on the product molecular weight 406.36. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for CHR 6494 trifluoroacetate
References for CHR 6494 trifluoroacetate
References are publications that support the biological activity of the product.
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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Citations for CHR 6494 trifluoroacetate
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.