Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CHR-6494 is a haspin inhibitor that inhibits histone H3T3 phosphorylation (IC50: 2 nM).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 229 | 现货 | ||
5 mg | ¥ 497 | 现货 | ||
10 mg | ¥ 957 | 现货 | ||
25 mg | ¥ 1,660 | 现货 | ||
50 mg | ¥ 2,470 | 现货 | ||
100 mg | ¥ 3,650 | 现货 | ||
200 mg | ¥ 5,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 559 | 现货 |
产品描述 | CHR-6494 is a haspin inhibitor that inhibits histone H3T3 phosphorylation (IC50: 2 nM). |
靶点活性 | Haspin: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]. |
分子量 | 292.34 |
分子式 | C16H16N6 |
CAS No. | 1333377-65-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (171.03 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.4207 mL | 17.1034 mL | 34.2067 mL | 85.5169 mL |
5 mM | 0.6841 mL | 3.4207 mL | 6.8413 mL | 17.1034 mL | |
10 mM | 0.3421 mL | 1.7103 mL | 3.4207 mL | 8.5517 mL | |
20 mM | 0.171 mL | 0.8552 mL | 1.7103 mL | 4.2758 mL | |
50 mM | 0.0684 mL | 0.3421 mL | 0.6841 mL | 1.7103 mL | |
100 mM | 0.0342 mL | 0.171 mL | 0.3421 mL | 0.8552 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CHR-6494 1333377-65-3 Others CHR6494 CHR 6494 Inhibitor inhibitor inhibit