A selective Haspin protein kinase inhibitor
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CHR-6494

Item No. 11478

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(1H-indazol-5-yl)-N-propyl-imidazo[1,2-b]pyridazin-6-amine
CAS Number
1333377-65-3
Molecular Formula
C16H16N6
Formula Weight
292.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12.5 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 0.25 mg/ml
λmax
213, 252, 335 nm
SMILES
CCCNC(C=C1)=NN2C1=NC=C2C3=CC(C=NN4)=C4C=C3
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $103

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    10 mg

    $183

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    Product 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huertas, D., Soler, M., Moreto, J., et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene 1-11 (2011).