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CHR6494 trifluoroacetate

Chemical Structure : CHR6494 trifluoroacetate

CAS No.: 1458630-17-5

CHR6494 trifluoroacetate (CHR6494 TFA)

Catalog No.: PC-49322Not For Human Use, Lab Use Only.

CHR-6494 (CHR6494) trifluoroacetate is a potent, selective inhibitor of the histone kinase Haspin with IC50 of 2 nM, shows anti-proliferative effects in human cancer cells.

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Biological Activity

CHR-6494 (CHR6494) trifluoroacetate is a potent, selective inhibitor of the histone kinase Haspin with IC50 of 2 nM, shows anti-proliferative effects in human cancer cells.
CHR-6494 displays selectivity over 27 other protein kinases including Aurora B kinase.
CHR-6494 inhibits cancer cell growth dose dependently with IC50 500 nM for HCT-116, 473 nM for HeLa and 752 nM for MDA-MB-231 cells.
CHR-6494 reduces H3T3ph levels in a dose-dependent manner and causes a mitotic catastrophe characterized by metaphase misalignment, spindle abnormalities and centrosome amplification.
CHR-6494 causes arrest in G2/M and subsequently apoptosis in cancer cells.
CHR-6494 demonstrates anti-angiogenetic features in ex vivo assays, shows antitumor potential in xenografted nude mice without any observed toxicity in vivo.

Physicochemical Properties

M.Wt 406.369
Formula C18H17F3N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(1H-indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine trifluoroacetate

References

1. Huertas D, et al. Oncogene. 2012 Mar 15;31(11):1408-18.

2. Han L, et al. J Cancer. 2017 Aug 25;8(15):2933-2943.

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