Dimethylenastron
(Synonyms: 2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮) 目录号 : GC32969
An inhibitor of EG5
Cas No.:863774-58-7
Sample solution is provided at 25 µL, 10mM.
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Dimethylenastron is an inhibitor of the mitotic kinesin Eg5 (IC50 = 200 nM in an ATPase assay).1 It is selective for Eg5 over other kinesin subfamilies from four different organisms. Dimethylenastron induces accumulation of HeLa cells in the G2/M phase (75% at a concentration of 1 μM). It inhibits spindle formation and induces radial arrangement of chromosomes in Xenopus oocytes. Dimethylenastron inhibits migration and growth of PANC-1 pancreatic cancer cells in a concentration-dependent manner.2 Dimethylenastron also inhibits angiogenesis and induces severe circulation defects in zebrafish embryos.3
1.Gartner, M., Sunder-Plassmann, N., Seiler, J., et al.Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5Chembiochem6(7)1173-1177(2005) 2.Sun, X.-d., Shi, X.-j., Sun, X.-o., et al.Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5Acta Pharmacol. Sin.32(12)1543-1548(2011) 3.Exertier, P., Javerzat, S., Wang, B., et al.Impaired angiogenesis and tumor development by inhibition of the mitotic kinesin Eg5.Oncotarget4(12)2302-2316(2013)
Cell experiment: | Cell invasion in response to Dimethylenastron is carried out by transwell assays. The upper surface of the transwell filters is coated with matrigel or fibronectin. Cells suspended in 200 μL serum-free media are added to the chamber, and the chamber is placed in a 24-well plate containing complete medium. After 24 h of incubation at 37°C, the filters are gently taken out and matrigel on the upper surface of the filters is removed by cotton swabs. Cells on the underside of transwell filters are fixed with 4% paraformaldehyde for 30 min, stained with 0.1% crystal violet for 10 min, and then photographed. For quantitative assessment, the number of invading cells is counted in five random fields per filter. The extent of cell invasion is quantified as the number of invading cells in the drug-treatment group divided by the number of invading cells in the control group[2]. |
Animal experiment: | Just after the conjunctival suture is closed, a metallic needle (30 G) is inserted into the subconjunctival space at the nasal margin of the superior rectus muscle and injection of one of the following agents is delivered: The rabbits receive either no adjuvant after the surgery in the control group, one unilateral subconjunctival injection of Dimethylenastron (1.0 µmol, 3.0 µmol) or of the vehicle (DMSO, 99.9%, 10 mg/mL) alone at baseline, which means an injection directly after surgery and in two further groups additionally at days 3 and 7 thereafter (1.0 µmol, 3.0 µmol)[3]. |
References: [1]. Gartner M, et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7. | |
| Cas No. | 863774-58-7 | SDF | |
| 别名 | 2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮 | ||
| Canonical SMILES | O=C1C2=C(NC(NC2C3=CC=CC(O)=C3)=S)CC(C)(C)C1 | ||
| 分子式 | C16H18N2O2S | 分子量 | 302.39 |
| 溶解度 | DMSO : ≥ 31 mg/mL (102.52 mM) | 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 | 3.307 mL | 16.5349 mL | 33.0699 mL |
| 5 mM | 0.6614 mL | 3.307 mL | 6.614 mL |
| 10 mM | 0.3307 mL | 1.6535 mL | 3.307 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet