Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MLN8054是一种有口服活性的高选择性极光激酶抑制剂,IC50值为4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 363 | 现货 | ||
2 mg | ¥ 619 | 现货 | ||
5 mg | ¥ 892 | 现货 | ||
10 mg | ¥ 1,320 | 现货 | ||
25 mg | ¥ 2,480 | 现货 | ||
50 mg | ¥ 3,980 | 现货 | ||
100 mg | ¥ 5,670 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 956 | 现货 |
产品描述 | MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM. |
靶点活性 | Aurora A:4 nM |
体外活性 | MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase with an IC50 of 4 nM, which shows >40-fold more selective inhibitory activity for Aurora A compared with Aurora B. [1] In vitro, MLN8054 exhibits the activity of growth inhibition across various cell lines from diverse tissue origins with IC50 values ranging from 0.11 μM to 1.43 μM. In addition, MLN8054 selectively inhibits Aurora A over Aurora B in cultured cells, and inhibits cell proliferation by promoting G2/M accumulation and spindle defects in multiple cultured human tumor cells lines. [1] A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks. [2] |
体内活性 | In the HCT-116 tumor-bearing mice, MLN8054, administered orally at 3 mg/kg, 10 mg/kg, and 30 mg/kg once a day, leads to dose-dependent tumor growth inhibition (TGI: 76% and 84% for 10 mg/kg and 30 mg/kg). MLN8054 also shows similar antitumor activity in the PC-3 tumor xenograft in nude mice. [1] In the HCT-116 xenograft-bearing animals, MLN8054 induces DNA and tubulin staining of tumor tissue in nuclear and cell body area, consistent with a senescent phenotype by increasing senescence-associated beta-galactosidase activity. [3] |
激酶实验 | Enzyme Assays : Recombinant murine Aurora A and Aurora B protein are expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A is conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) is assayed in 50 mM Hepes (pH 7.5)/10 mM MgCl2/5 mM DTT/0.05% Tween 20/2 μM peptide substrate/3.3 μCi/ml [γ-33P]ATP at 2 μM by using Image FlashPlates. Aurora B kinase (2 nM) is assayed with 10 μM biotinylated peptide Biotin-TKQTARKSTGGKAPR in 50 mM Tricine (pH 8.0)/2.5 mM MgCl2/5 mM DTT/10% glycerol/2% BSA/40 μCi/ml [γ-33P]ATP at 250 μM. The conditions for all other in vitro kinase assays are available upon request. MLN8054 is run in a 226 kinase screen at a 1 μM compound concentration with an ATP concentration of 10 μM for all assays. |
细胞实验 | Human tumor cell lines are grown in 96-well cell culture dishes according to the distributor's recommendations. MLN8054, diluted in DMSO, is added to the cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 mM to 0.04 mM. MLN8054 at each dilution is added in triplicate with each replicate on a separate plate. Cells treated with DMSO (n = 6 wells per plate; 0.2% final concentration) serves as the untreated control. The cells are treated with MLN8054 for 96 hours at 37 °C in a humidified cell culture chamber. Cell viability in each cell line is measured by using the Cell Proliferation ELISA, BrdU colorimetric kit according to the manufacturer's recommendation(Only for Reference) |
分子量 | 476.86 |
分子式 | C25H15ClF2N4O2 |
CAS No. | 869363-13-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 88 mg/mL (184.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0971 mL | 10.4853 mL | 20.9705 mL | 52.4263 mL |
5 mM | 0.4194 mL | 2.0971 mL | 4.1941 mL | 10.4853 mL | |
10 mM | 0.2097 mL | 1.0485 mL | 2.0971 mL | 5.2426 mL | |
20 mM | 0.1049 mL | 0.5243 mL | 1.0485 mL | 2.6213 mL | |
50 mM | 0.0419 mL | 0.2097 mL | 0.4194 mL | 1.0485 mL | |
100 mM | 0.021 mL | 0.1049 mL | 0.2097 mL | 0.5243 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。
MLN8054 869363-13-3 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Metabolism Stem Cells Tyrosine Kinase/Adaptors Aurora Kinase Src PKA Casein Kinase inhibit MLN-8054 MLN 8054 Inhibitor inhibitor