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CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA induces cell cycle arrest at G2/M, inhibits cell proliferation, and promotes apoptosis in multiple cancer cell lines. CHR-6494 TFA inhibits histone H3T3 phosphorylation.
CHR-6494 TFA (500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1. CHR-6494 TFA (200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237.
CHR-6494 TFA (50 mg/kg; i.p.; in two cycles of five consecutive days for 15 days) inhibits the growth of tumor in nude mice bearing HCT-116 human colorectal cancer cells. CHR-6494 TFA (20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor growth in nude mice bearing MDA-MB-231 xenograft tumors.
| Molecular Weight | 406.36 |
| Formula | C18H17F3N6O2 |
| CAS Number | 1458630-17-5 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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