Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MPI0479605 是一种选择性的,ATP 竞争性的 Mps1抑制剂,IC50值为 1.8 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 733 | 现货 | ||
2 mg | ¥ 987 | 现货 | ||
5 mg | ¥ 1,530 | 现货 | ||
10 mg | ¥ 2,770 | 现货 | ||
25 mg | ¥ 4,590 | 现货 | ||
50 mg | ¥ 6,580 | 现货 | ||
100 mg | ¥ 8,960 | 现货 | ||
500 mg | ¥ 17,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,530 | 现货 |
产品描述 | MPI-0479605 is an ATP competitive and selective inhibitor. |
靶点活性 | Mps1:1.8 nM |
体外活性 | 在肠癌移植模型中,每天30 mg/kg或者每4天150 mg/kg腹腔注射MPI-0479605,具有抗肿瘤活性. |
体内活性 | 在一组肿瘤细胞系中,MPI-0479605导致细胞活力显著降低,GI50范围为30至100 nM。此外,MPI-0479605通过凋亡或者有丝分裂损伤来诱发细胞生长阻滞并最终促进细胞死亡。MPI-0479605破坏SAC和染色体在有丝分裂纺锤体上的附着,进而导致染色体分离缺陷和异倍体。 |
激酶实验 | In Vitro Kinase Assays and Selectivity Screening : To measure Mps1 activity, 25 ng of recombinant, full-length enzyme is incubated in reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.01% Triton X-100 and 5 μM Myelin basic protein (MBP)) containing vehicle (DMSO alone) or inhibitors. Forty μM ATP (2xKm) is added with 1 μCi [γ-33P]ATP and the reaction is incubated at room temperature for 45 minutes. Reactions are terminated with 3% phosphoric acid and transferred to P81 filter plates. Samples are washed in 1% phosphoric acid and 33P radioactivity is measured on a TopCount scintillation reader. In-house kinase assays are all carried out at 2xKm ATP concentrations. MPI-0479605 (500 nM) is also screened against a larger kinase panel. |
细胞实验 | Cells are treated for 3 or 7 days with various concentrations of MPI-0479605 and the GI50 is determined. Cell viability is measured with CellTiter-Glo. (Only for Reference) |
分子量 | 407.51 |
分子式 | C22H29N7O |
CAS No. | 1246529-32-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 58 mg/mL (142.3 mM)
Ethanol: 2 mg/mL (4.9 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.4539 mL | 12.2696 mL | 24.5393 mL | 61.3482 mL |
DMSO | 5 mM | 0.4908 mL | 2.4539 mL | 4.9079 mL | 12.2696 mL |
10 mM | 0.2454 mL | 1.227 mL | 2.4539 mL | 6.1348 mL | |
20 mM | 0.1227 mL | 0.6135 mL | 1.227 mL | 3.0674 mL | |
50 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 1.227 mL | |
100 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6135 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。
MPI-0479605 1246529-32-7 Apoptosis Cytoskeletal Signaling Kinesin Monopolar spindle 1 Inhibitor MPI 0479605 MPI0479605 inhibit Mps1 inhibitor