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MLN8054

MLN8054

产品编号 T6315   CAS 869363-13-3

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。

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MLN8054 Chemical Structure
MLN8054, CAS 869363-13-3
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
其他形式的 MLN8054:
产品目录号及名称: MLN8054 (T6315)
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纯度: 99.05%
纯度: 98.26%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 88 mg/mL (184.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Manfredi MG, et al. Proc Natl Acad Sci U S A, 2007, 104(10), 4106-4111. 2. Moretti L, et al. Int J Radiat Oncol Biol Phys, 2011, 80(4), 1189-1197. 3. Huck JJ, et al. Mol Cancer Res, 2010, 8(3), 373-384.

文献引用

1. Li Y, Tang S, Shi X, et al.Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer.Cell Reports Medicine.2023
LY294002 Ac-VDVAD-CHO Ellagic acid BioE-1115 Casein Kinase II Inhibitor IV IWP-2 AS-252424 SSTC3

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 酪氨酸激酶分子库 抗癌活性化合物库 抗癌临床化合物库 高选择性抑制剂库 抗胰腺癌化合物库 抗衰老化合物库 含氟化合物库 抗癌细胞代谢库 代谢化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
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技术支持

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。

Keywords

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

 

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