372040

Haspin Kinase Inhibitor, CHR-6494

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₆H₁₆N₆
• CAS-Nummer: 1333377-65-3
• Molekulargewicht: 292.34
• MDL number: MFCD22666352
• UNSPSC Code: 12352200
• NACRES: NA.54
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Eigenschaften

• assay: ≥98% (HPLC)
• Quality Segment: 100
• 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
• 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

Beschreibung

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.).

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.

Other Notes

Huertas, D., et al. 2012. Oncogene31, 1408.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable