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CHR 6494 trifluoroacetate
Axon 2250
- Parent CAS: 1333377-65-3
Purity:
99%
- Soluble in DMSO
- MF: C16H16N6.C2HF3O2
- MW: 406.36
Description
CHR 6494 trifluoroacetate is a first-in-class inhibitor of the mitotic kinase Haspin that blocks histone H3 threonine-3 phosphorylation and produces spindle and centrosome phenotypes. It induces G2/M arrest and apoptosis in tumor-cell models, with reported apoptosis-induction IC50 values of 500 nM, 473 nM and 752 nM in HCT-116, HeLa and MDA-MB-231 cells.
Haspin activity supports chromosome cohesion, metaphase alignment and mitotic progression. CHR 6494 is a valuable probe for investigating mitotic kinase biology, chromosome-segregation defects and anti-proliferative cancer mechanisms.
Key Features
- First-in-class Haspin kinase inhibitor
- Blocks histone H3T3 phosphorylation
- Induces G2/M arrest and apoptosis
- Produces spindle and centrosome defects
Applications
- Mitotic kinase research
- Cell-cycle and chromosome-alignment studies
- Cancer-cell apoptosis assays
- Anti-angiogenesis and tumor model studies
More Information
| Parent CAS No. | 1333377-65-3 |
|---|---|
| Chemical Name | 3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine trifluoroacetate |
| SMILES | CCCNC1=NN2C(C3C=CC4NN=CC=4C=3)=CN=C2C=C1.OC(C(F)(F)F)=O |
| MFCD | N.A. |
| InChi | InChI=1S/C16H16N6.C2HF3O2/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;3-2(4,5)1(6)7/h3-6,8-10H,2,7H2,1H3,(H,17,21)(H,19,20);(H,6,7) |
| InChiKey | ILWYDZNXJQESDI-UHFFFAOYSA-N |
| CID | 91691123 |
| Short Description | Haspin inhibitor |
CHR 6494 trifluoroacetate
first-in-class Haspin kinase inhibitor
CHR6494
Histone
H3T3
G2/M
first-in-class Haspin kinase
Inhibitor
Mitotic kinase research
Cell-cycle and chromosome-alignment studies
Cancer-cell apoptosis assays
Anti-angiogenesis and tumor model studies
apoptosis
cell cycle
angiogenesis
cancer biology
kinase signaling
drug discovery
Axon Medchem
Axon 2250
Supplier
Vendor
References
- Huertas, D. et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene (2012), 31(11), 1408-1418.
- Cuny, Gregory D. et al. Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Bioorg. Med. Chem. Lett. 2012, 22, 2015-2019.
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