| Description | CHR-6494 TFA is a potent haspin inhibitor, with an IC50 of 2 nM. It inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer |
| In vitro | CHR-6494（TheaflavinA；0-10-5nM；72小时）的给药能剂量依赖性地抑制癌细胞生长，包括HCT-116、HeLa、MDA-MB-231和Wi-38细胞，其IC50分别为500nM、473nM、752nM和1059nM[1]。CHR-6494（TheaflavinA；500nM）的给药能导致有丝分裂灾难，包括有丝分裂纺锤体和中心体形态异常放大，同时上调纺锤体组装检查点蛋白BUB1和有丝分裂停滞标记蛋白cyclin B1[1]。 |
| In vivo | 给予CHR-6494 （TFA；50mg/kg；腹腔注射，两个周期，每周期五连续天，共15天）能抑制裸鼠体内携带HCT-116人类结直肠癌细胞的肿瘤生长，并未观察到明显的体重变化[1]。 |
| Target activity | Haspin:2 nM (IC50) |
| molecular weight | 406.36 |
| Molecular formula | C18H17F3N6O2 |
| CAS | 1458630-17-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 55 mg/mL (135.35 mM) |
| References | 1. Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18. |