Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,260 | 4-5周 | ||
5 mg | ¥ 5,510 | 4-5周 | ||
10 mg | ¥ 9,620 | 4-5周 |
产品描述 | EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM). |
靶点活性 | Kinesin-5:8 nM |
体外活性 | EMD 534085 does not inhibit any other tested kinesins at 1 μM or 10 μM concentration, showing selectively over kinesin-5. EMD 534085 binds to the allosteric pocket of kinesin-5 [1]. EMD534085 induces rapid cell death in HL60 during mitotic arrest. Caspase-8, ?9, ?3, ?7 are activated; Parp1 is cleaved; Mcl1 and XIAP are degraded in EMD534085-treated HL60 cells. EMD534085 treated HL60 cells also show significantly accumulated phospho-histone H3 level starting at 6 hrs post thymidine release [2]. |
体内活性 | In a low dose PK of EMD 534085 in mice, the clearance is 1.8 L/h/kg on average, the volume of distribution is 7.4 L/kg and the half-life around 2.5 h. The bioavailability in high dose experiments (>10 mg/kg) is always above 50% in mice. Intraperitoneal administration of EMD 534085 enables significant systemic exposure in mice leading to a significant tumor growth reduction without toxic side effects [1]. |
细胞实验 | Epithelial cell lines HeLa and MCF7 are synchronized in G2-phase using RO-3306. Cells are treated with 10 μM RO-3306 for 16 hrs, and then are ished and released to either warm growth medium or medium supplemented with 500 nM EMD534085 [2]. |
分子量 | 476.53 |
分子式 | C25H31F3N4O2 |
CAS No. | 858668-07-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (52.46 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0985 mL | 10.4925 mL | 20.985 mL | 52.4626 mL |
5 mM | 0.4197 mL | 2.0985 mL | 4.197 mL | 10.4925 mL | |
10 mM | 0.2099 mL | 1.0493 mL | 2.0985 mL | 5.2463 mL | |
20 mM | 0.1049 mL | 0.5246 mL | 1.0493 mL | 2.6231 mL | |
50 mM | 0.042 mL | 0.2099 mL | 0.4197 mL | 1.0493 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。
EMD534085 858668-07-2 Cytoskeletal Signaling Kinesin EMD-534085 EMD 534085 Inhibitor inhibitor inhibit