化合物 T14959 T14959

Product Introduction
Bioactivity


英文名: CHR-6494

描述: CHR-6494 is a haspin inhibitor that inhibits histone H3T3 phosphorylation (IC50: 2 nM).

体外活性: CHR-6494 does not modify H3S10 and H328 phosphorylation levels and shows no significantly inhibitory effects on other protein kinases. CHR-6494 dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cell (IC50s: 500?nM, 473?nM, 752?nM, and 1059 nM). CHR-6494 (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 [1]. CHR-6494 exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM. CHR-6494 (300 nM and 600 nM) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 cells. CHR-6494 in combination with MEK inhibitors synergistically inhibits the viability of melanoma cells, enhances apoptosis in melanoma cells, modulates cell cycle progression independently by arresting melanoma cells at different phases, and suppresses migration of melanoma cells [2].

体内活性: CHR-6494 (50?mg/kg, i.p.) inhibits the growth of tumor. It cuases no obvious body weight change in nude mice bearing HCT-116 human colorectal cancer cells [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (171.03 mM)


关键字: CHR6494 | CHR-6494 | CHR 6494

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途