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Alisertib

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产品编号 T2241Cas号 1028486-01-2
别名 MLN 8237, 4-[[9-氯-7-(2-氟-6-甲氧基苯基)-5H-嘧啶并[5,4-D][2]苯并氮杂卓-2-基]氨基]-2-甲氧基苯甲酸

Alisertib (MLN 8237) 是一种 Aurora A 激酶抑制剂 (IC50=1.2 nM),具有口服活性和选择性。Alisertib 具有抗肿瘤活性,可以诱导细胞凋亡和自噬,诱导细胞周期阻滞。

Alisertib

Alisertib

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纯度: 100%
产品编号 T2241 别名 MLN 8237, 4-[[9-氯-7-(2-氟-6-甲氧基苯基)-5H-嘧啶并[5,4-D][2]苯并氮杂卓-2-基]氨基]-2-甲氧基苯甲酸Cas号 1028486-01-2

Alisertib (MLN 8237) 是一种 Aurora A 激酶抑制剂 (IC50=1.2 nM),具有口服活性和选择性。Alisertib 具有抗肿瘤活性,可以诱导细胞凋亡和自噬,诱导细胞周期阻滞。

规格价格库存数量
1 mg¥ 248现货
5 mg¥ 578现货
10 mg¥ 813现货
25 mg¥ 1,490现货
50 mg¥ 2,450现货
100 mg¥ 3,180现货
200 mg¥ 5,120现货
500 mg¥ 7,890现货
1 mL x 10 mM (in DMSO)¥ 663现货
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产品介绍

生物活性
产品描述
Alisertib (MLN 8237) is an Aurora A kinase inhibitor (IC50=1.2 nM) with oral activity and selectivity. Alisertib has antitumor activity, induces apoptosis and autophagy, and induces cell cycle arrest.
靶点活性
Aurora A:1.2 nM (cell free)
体外活性
方法:从 MM 患者获得的一组 MM 细胞系和肿瘤细胞用 Alisertib (0.0001-4 µM) 处理 48-72 h,使用 MTT assay 检测细胞活力。
结果:尽管 Alisertib 的细胞毒性活性早在暴露于低于 0.1 µM/L 的 24-48 h 就在几种细胞系中检测到了,但在所有细胞系中,在 72 h 时都发生了更强烈的细胞毒性。[1]
方法:人结直肠癌细胞 HCT-116 用 Alisertib (0.05-1 µmol/L) 处理 24-48 h,使用 Flow cytometry 检测细胞周期。
结果:在浓度为 0.050 µmol/L 时,在 24 和 48 h 时,G2/M 期的细胞增加,表型与 Aurora A 抑制一致。在 0.250 和 1.000 µmol/L 的较高浓度下,Alisertib 处理的细胞显示出与 Aurora B 抑制一致的表型,显示 8N DNA 含量的细胞数量增加。[2]
体内活性
方法:为研究抗肿瘤活性,将 Alisertib (7.5-30 mg/kg,10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate) 口服给药给携带 MM1.S 异种移植物的 SCID 小鼠,每天一次,持续二十一天。
结果:用 30 mg/kg Alisertib 治疗的动物的肿瘤负荷显著降低。与对照相比,15 mg/kg (TGI=42%) 和 30 mg/kg (TGI=80%) 处理的动物的 TGI 显著。[1]
激酶实验
Recombinant murine Aurora A and Aurora B protein were expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A was conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) was 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) was 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 was run in a 226 kinase screen at a 1 μM compound concentration with an ATP concentration of 10 μM for all assays [2].
细胞实验
HCT-116 colorectal carcinoma cells were plated on 6-well dishes (2 × 10^5 per well) and propagated in McCoy's 5A media supplemented with 10% FBS. After 18 hours, alisertib at a final concentration of 0.050, 0.250, or 1.000 μmol/L was added, and the cells were grown for an additional 24 hours. Cells treated with dimethyl sulfoxide (DMSO; 0.2%) served as the untreated vehicle control. The cells were harvested with trypsin EDTA 1×, washed once with PBS, fixed in 70% ethanol, and stored at 4°C for 1 hour. The cells were resuspended in propidium iodide (1:40) and RNAse A (1:5,000) in PBS for 30 minutes at 4°C. Cell-cycle distributions were determined by measuring DNA content using flow cytometry, and samples were analyzed using Winlist 5.0 software [2].
动物实验
Mice were irradiated (200 cGy), and then 5 × 106 MM1.S cells were inoculated subcutaneously in the right flank. When tumor growth was measurable (~ 2 weeks after the injection), mice were assigned into 4 groups (10 mice each) receiving vehicle orally (100 μL of 10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate) or MLN8237 (7.5 mg/kg, 15 mg/kg, and 30 mg/kg in a final formulation in 10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate) for 21 consecutive days. The maximal tolerated dose of MLN8237 in most mouse strains (continuous dosing for 21 days) is approximately 20 mg/kg twice a day (40 mg/kg per day). Tumor volumes were measured by a Vernier caliper every alternate day and calculated using the following formula: length × width2 × 0.5. Tumor growth inhibition (TGI) was calculated using the formula (Δcontrol average volume ? Δtreated average volume) × 100/(Δcontrol average volume). Mice were killed at the end of the treatment, 2 hours after the last treatment, or when tumor reached 2 cm^3; tumors were immediately collected from mice and evaluated for induction of apoptosis and cell death by TdT-mediated dUTP nick end labeling (TUNEL) assay [1].
别名MLN 8237, 4-[[9-氯-7-(2-氟-6-甲氧基苯基)-5H-嘧啶并[5,4-D][2]苯并氮杂卓-2-基]氨基]-2-甲氧基苯甲酸
化学信息
分子量518.92
分子式C27H20ClFN4O4
CAS No.1028486-01-2
SmilesCOc1cc(Nc2ncc3CN=C(c4cc(Cl)ccc4-c3n2)c2c(F)cccc2OC)ccc1C(O)=O
密度1.438 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.64 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO: 50 mg/mL (96.35 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
1mg5mg10mg50mg
1 mM1.9271 mL9.6354 mL19.2708 mL96.3540 mL
5 mM0.3854 mL1.9271 mL3.8542 mL19.2708 mL
1mg5mg10mg50mg
10 mM0.1927 mL0.9635 mL1.9271 mL9.6354 mL
20 mM0.0964 mL0.4818 mL0.9635 mL4.8177 mL
50 mM0.0385 mL0.1927 mL0.3854 mL1.9271 mL

计算器

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  • 稀释 计算器
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  • 分子量 计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 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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