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| | CHR-6494 Basic information |
| Product Name: | CHR-6494 | | Synonyms: | 3-(1H-indazol-5-yl)-N-propyliMidazo[1,2-b]pyridazin-6-aMine;CHR-6494 3-(1H-indazol-5-yl)-N-propyliMidazo[1,2-b]pyridazin-6-aMine;3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt;3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt;CHR 6494 trifluoroacetate salt;CHR-6494 trifluoroacetate salt;Haspin Kinase Inhibitor, CHR-6494;CHR-6494 | | CAS: | 1333377-65-3 | | MF: | C16H16N6 | | MW: | 292.34 | | EINECS: | | | Product Categories: | | | Mol File: | 1333377-65-3.mol |  |
| | CHR-6494 Chemical Properties |
| density | 1.39±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble5mg/mL, clear (warmed) | | pka | 13.24±0.40(Predicted) | | form | powder | | color | white to beige |
| | CHR-6494 Usage And Synthesis |
| Description | CHR-6494 is a haspin protein kinase inhibitor (IC50 = 2 nM) selective over 27 other protein kinases, including Aurora B kinase (IC50 > 1 μM). Haspin is a kinase necessary for mitosis that selectively phosphorylates histone 3 at the threonine 3 residue (H3T3ph). CHR-6494 decreases phosphorylation of H3T3 and arrests the cell cycle in the G2/M phase, which leads to apoptosis. It showed promising results in a xenograft tumor model. | | Uses | CHR6494 is a small-molecule inhibitor of histone kinase haspin, with a wide spectrum of anticancer effects. | | General Description | A cell-permeable indazolylimidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC50 = 2 nM) with moderate selectivity over TrkA, GSK-3β, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100 nM = 58, 48, 36, 34 and 33, respectively) among a panel of 27-kinases. Shown to block pH3-Thr3, with no effect on pH3-Ser10 and pH3-Ser28, cause mitotic catastrophe, upregulate BUB1 and cyclin B1 levels, and potently induce apoptosis (IC50 = 473, 500 and 752 nM in HeLa, HCT-116 and MDA-MB-231 cells, respectively). Further, efficiently blocks bFGF-induced sprouting vessel by 70% at 1 μM (chicken embryo aortic arch ring assay) and suppresses tumor growth in HCT-116 xenografted mouse model (50 mg/kg, i.p.). |
| | CHR-6494 Preparation Products And Raw materials |
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