| Identification | Back Directory | [Name]
CHR-6494 | [CAS]
1333377-65-3 | [Synonyms]
CS-609
CHR-649
CHR-6494
CHR 6494;CHR6494
CHR 6494 trifluoroacetate salt
CHR-6494 trifluoroacetate salt
Haspin Kinase Inhibitor, CHR-6494
3-(1H-indazol-5-yl)-N-propyliMidazo[1,2-b]pyridazin-6-aMine
Imidazo[1,2-b]pyridazin-6-amine, 3-(1H-indazol-5-yl)-N-propyl-
Haspin Kinase Inhibitor, CHR-6494 - CAS 1333377-65-3 - Calbiochem
3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt
3-(1H-Indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine trifluoroacetate salt
CHR-6494 3-(1H-indazol-5-yl)-N-propyliMidazo[1,2-b]pyridazin-6-aMine | [Molecular Formula]
C16H16N6 | [MDL Number]
MFCD24849399 | [MOL File]
1333377-65-3.mol | [Molecular Weight]
292.34 |
| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL, clear (warmed) | [form ]
powder | [pka]
13.24±0.40(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [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).1 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.). |
|
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
|