Chemical Structure : CHR6494 trifluoroacetate
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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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.
M.Wt | 406.369 | |
Formula | C18H17F3N6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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