CHR-6494 is a potent and selective Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor that blocks H3T3ph phosphorylation.
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描述 | CHR-6494 is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer[1]. |
体内研究 | Administration of CHR-6494 at doses of 50 mg/kg intraperitoneally in two cycles of five consecutive days for 15 days inhibits tumor growth without causing significant changes in body weight in nude mice bearing HCT-116 human colorectal cancer cells [1]. Moreover, CHR-6494 at a dose of 20 mg/kg via intraperitoneal injection for 15 consecutive days inhibits tumor volume and weight compared to the control group in nude mice bearing MDA-MB-231 xenograft tumors [3]. Additionally, CHR-6494 at a dose of 20 mg/kg via intraperitoneal injection for 15 consecutive days enhances the inhibition of tumor volume and weight when combined with MLN8237 (20 mg/kg orally) in vivo [3]. |
体外研究 | Treatment with CHR-6494 at concentrations ranging from 0 to 500 nM for 72 hours results in a dose-dependent inhibition of cancer cell growth, including HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC50s of 500 nM, 473 nM, 752 nM, and 1059 nM, respectively [1]. At a concentration of 500 nM, CHR-6494 induces mitotic catastrophe characterized by abnormal morphology of the mitotic spindle and centrosome amplification. It also upregulates the spindle assembly checkpoint protein BUB1 and the mitotic arrest marker cyclin B1 [1]. Moreover, 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 [2]. Treatment with CHR-6494 at concentrations of 300 nM and 600 nM for 72 hours induces apoptosis, increasing caspase 3/7 activity by 3- and 6-fold, respectively, in COLO-792 cells and by 8.5- and 16-fold in RPMI-7951 cells [2]. Furthermore, CHR-6494 synergistically enhances the viability inhibition and apoptosis induction of melanoma cells in combination with MEK inhibitors. It also modulates cell cycle progression independently by arresting melanoma cells at different phases and suppresses melanoma cell migration [2]. Treatment with CHR-6494 at the concentration of 50- 200 nM for 1 week enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells[3]. Treatment with CHR-6494 at the concentration of 50- 200 nM for 72 hours enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.42mL 0.68mL 0.34mL |
17.10mL 3.42mL 1.71mL |
34.21mL 6.84mL 3.42mL |
CAS号 | 1333377-65-3 |
分子式 | C16H16N6 |
分子量 | 292.338 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 50 mg/mL(171.03 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |