372040
Haspin Kinase Inhibitor, CHR-6494
别名:
Haspin Kinase Inhibitor, CHR-6494, Indazolyl-propylimidazopyridazin-amine, 3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine, Haploid Germ Cell-Specific Nuclear Protein Kinase Inhibitor, CHR-6494
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关于此项目
经验公式（希尔记法）:
C16H16N6
化学文摘社编号:
分子量:
292.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.54
SMILES string
[n]21nc(ccc2ncc1c3cc4c([nH]nc4)cc3)NCCC
InChI
1S/C16H16N6/c1-2-7-17-15-5-6-16-18-10-14(22(16)21-15)11-3-4-13-12(8-11)9-19-20-13/h3-6,8-10H,2,7H2,1H3,(H,17,21)(H,19,20)
InChI key
CZZCAOGIEGXMBZ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 25 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
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.).
Other Notes
Huertas, D., et al. 2012. Oncogene31, 1408.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Hisayo Nishida-Fukuda et al.
PloS one, 16(4), e0249912-e0249912 (2021-04-15)
HASPIN is a serine/threonine kinase that regulates mitosis by phosphorylating histone H3 at threonine 3. The expression levels of HASPIN in various cancers are associated with tumor malignancy and poor survival, suggesting that HASPIN inhibition may suppress cancer growth. As
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