SBE 13 HCl
目录号 : GC14644
A potent Plk1 inhibitor
Cas No.:1052532-15-6
Sample solution is provided at 25 µL, 10mM.
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The serine/threonine kinase polo-like kinase 1 (Plk1) attracts great attention in the field of cancer therapy because it exhibits generally elevated activity in cancer cells and is a negative prognostic factor for cancer patients. The importance of Plk1 activity as a measure for the aggressiveness of a tumor results from its important role in mitotic checkpoints. SBE13 is identified as a novel and potent inhibitor of inactive Plk1.
In vitro: To determine its ability to induce cell death in cancer cells, we applied kinase assays, western blot analyses, FACS can analyses, Caspase assays and immunofluorescence studies. We detected decreased cell proliferation, delayed progression through the cell cycle in lower SBE13 concentrations, a G2/M arrest using higher SBE13 concentrations followed by apoptosis, and abnormal mitotic figures. Notably, SBE13 did not influence activity of other kinases (Plk2, Plk3, Aurora A), indicating the selectivity of this type II Plk1 inhibitor [1].
In silico: The docking pose of SBE13 in the homology model suggests an interaction with Arg 95 of Plk1, and thus spans the whole hydrophobic pocket, which is anticipated for a type II inhibitor. Another SBE13’s characteristic feature of type II inhibitors is the interaction with the hinge region and with the Asp in the Asp-Phe-Gly (DFG) motif [2].
Clinical trial: Up to now, SBE13 is still in the preclinical development stage.
Reference:
[1] Keppner S, Proschak E, Kaufmann M, Strebhardt K, Schneider G, Sp?nkuch B. Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010 Feb 15;9(4):761-73.
[2] Keppner S, Proschak E, Schneider G, Sp?nkuch B. Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem. 2009 Nov;4(11):1806-9.
Kinase experiment: | To assay Plk1 kinase activity, cells are lysed after 13?h release in the presence of SBE13 after double thymidine block and kinase is immunoprecipitated from lysates using antibodies. In brief, for each immunoprecipitation 800?μg of total protein are incubated with Plk1 antibody cocktail (1.5?μg) for 2?h at 4°C on a rotator. Immunoprecipitated protein is collected using Protein A/G Agarose beads. Plk1 immunoprecipitates are incubated with casein (1?μg) and with [γ-32P]ATP (1?μCi) for 30?min at 37°C in kinase buffer. Products from the kinase assays are fractionated on 10?% bis-tris-polyacrylamide gels, and phosphorylated substrate is visualized by autoradiography after an exposure of 12-36?h. Equal amounts of immunoprecipitates are subjected to Western blot analysis to confirm equal loading of Plk1 protein in kinase reactions[1]. |
References: [1]. Keppner S, et al. Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem. 2009 Nov;4(11):1806-9. | |
| Cas No. | 1052532-15-6 | SDF | |
| 化学名 | N-(4-((6-chloropyridin-3-yl)methoxy)-3-methoxybenzyl)-2-(3,4-dimethoxyphenyl)ethanamine hydrochloride | ||
| Canonical SMILES | COC1=C(OC)C=C(CCNCC2=CC(OC)=C(OCC3=CN=C(Cl)C=C3)C=C2)C=C1.Cl | ||
| 分子式 | C24H28Cl2N2O4 | 分子量 | 479.4 |
| 溶解度 | DMF: 10 mg/ml,DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml,DMSO: 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0859 mL | 10.4297 mL | 20.8594 mL |
| 5 mM | 0.4172 mL | 2.0859 mL | 4.1719 mL |
| 10 mM | 0.2086 mL | 1.043 mL | 2.0859 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet