中文名称: | Dimethylenastron | ||||
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英文名称: | Dimethylenastron | ||||
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 2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone | ||||
CAS No: | 863774-58-7 | 分子式: | C16H18N2O2S | 分子量: | 302.39 |
CAS No: | 863774-58-7 | ||||
分子式: | C16H18N2O2S | ||||
分子量: | 302.39 |
基本信息
产品编号:D10040 |
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产品名称:Dimethylenastron |
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CAS: |
863774-58-7 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量: |
302.39 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
60mg/mL (198.41mM) |
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Ethanol |
1.5mg/mL (4.96mM) |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.3070mL |
16.5349mL |
33.0699mL |
5mM |
0.6614mL |
3.3070mL |
6.6140mL |
10mM |
0.3307mL |
1.6535mL |
3.3070mL |
50mM |
0.0661mL |
0.3307mL |
0.6614mL |
生物活性
产品描述 |
一种可逆的驱动蛋白(Eg5)抑制剂。 |
靶点/IC50 |
KSP |
200nM |
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体外研究 |
Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200nM.Dimethylenastron exhibits no inhibition of five other kinesin subfamilies (kinesin 1/4/7/10 and one ungrouped-originating from 4 different organisms). Dimethylenastron (0.5, 1μM) causes accumulation of cells in G2/M in HeLa cells. Dimethylenastron (3 and 10μM) concentration-dependently suppresses the migratory ability of the cancer cells in PANC1 pancreatic cancer cells after treatment for 24h, but does not inhibit the proliferation of cancer cells at 24h until 72h. Dimethylenastron also reduces invasion ability of the cancer cells. |
体内研究 |
Dimethylenastron (1.0µmol) induces a milder scarring but the length of bleb survival is not significantly prolonged compared with the control group. Dimethylenastron (1.0µmol) reveals a markedly reduced ratio of intraocular pressure and a milder, but not obviously reduced,subconjunctival fibrotic reaction in the rabbits treated with glaucoma filtration surgery. |
推荐实验方法(仅供参考)
细胞实验: |
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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 200μL serum-free media are added to the chamber, and the chamber is placed in a 24-well plate containing complete medium. After 24h of incubation at 37℃, 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. |
动物实验: |
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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 (1.0µmol,3.0µmol) or of the vehicle (DMSO, 99.9%, 10mg/mL) alone at baseline, which means an injection directly after surgery and in two further groups additionally at days 3 and 7 thereafter (1.0µmol,3.0µmol). |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )