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网站主页 化工产品目录 生物化工 抑制剂 细胞周期(Cell Cycle) Aurora Kinase 抑制剂 阿立塞替 化合物 Alisertib
  • 化合物 Alisertib|T2241

化合物 Alisertib|T2241

Alisertib
1028486-01-2
248 1mg 起订
578 5mg 起订
813 10mg 起订
上海 更新日期:2024-09-14

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产品详情:

中文名称:
化合物 Alisertib
英文名称:
Alisertib
CAS号:
1028486-01-2
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.82%
产品类别:
抑制剂
货号:
T2241

Product Introduction

Bioactivity

名称Alisertib
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.
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].
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].
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].
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]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度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)
关键字arrest | myeloma | MLN8237 | cytotoxicity | spindle | inhibit | mitotic | Autophagy | Aurora Kinase | cancer | multiple | Inhibitor | MLN-8237 | cell-cycle | Apoptosis | Alisertib
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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|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起,为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部,化学事业部,生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应;从商业化产品销售到个性化定制合成;从对明确靶点的分子筛选到对明确分子的多靶点筛选,从高通量筛选到化学结构优化,我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘,我们已成为筛选化合物领域优秀的供应商,为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

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