Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CX-6258是一种强效选择性的泛 Pim 激酶抑制剂,对Pim-1、Pim-2 和 Pim-3 作用的IC50值分别为 5、25 和 16 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 745 | 现货 | ||
10 mg | ¥ 1,190 | 现货 | ||
25 mg | ¥ 2,320 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 4,990 | 5日内发货 | ||
200 mg | ¥ 7,280 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity. |
靶点活性 | Pim3:16 nM, Pim1:5 nM, Pim2:25 nM |
体外活性 | CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. [1] |
激酶实验 | Pim activity assay: Pim-1 and Pim-2 inhibitions are measured in radiometric assays using human recombinant Pim-1 at [ATP] = 30 μM (substrate RSRHSSYPAGT) and human recombinant Pim-2 at [ATP] = 5 μM (substrate RSRHSSYPAGT). The radiometric assay for Pim-3 uses RSRHSSYPAGT as a substrate in the presence of [ATP] = 155 μM. |
别名 | CX 6258 |
分子量 | 461.94 |
分子式 | C26H24ClN3O3 |
CAS No. | 1202916-90-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (48.71 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1648 mL | 10.8239 mL | 21.6478 mL | 54.1196 mL |
5 mM | 0.433 mL | 2.1648 mL | 4.3296 mL | 10.8239 mL | |
10 mM | 0.2165 mL | 1.0824 mL | 2.1648 mL | 5.412 mL | |
20 mM | 0.1082 mL | 0.5412 mL | 1.0824 mL | 2.706 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。
CX-6258 1202916-90-2 Chromatin/Epigenetic JAK/STAT signaling Pim CX6258 Pim kinases Inhibitor inhibit Bad 4E-BP1 CX 6258 inhibitor