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372040

Haspin Kinase Inhibitor, CHR-6494

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C16H16N6
CAS Number:
1333377-65-3
Molecular Weight:
292.34
MDL number:
MFCD22666352
UNSPSC Code:
12352200
NACRES:
NA.54
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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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

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)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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