中文名称: Dimethylenastron
英文名称: Dimethylenastron
CAS No: 863774-58-7
分子式: C16H18N2O2S
分子量: 302.39
D10040 Dimethylenastron ≥98% (HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(15 mg/mL )
产品描述:

基本信息

产品编号:D10040

产品名称:Dimethylenastron

CAS:

863774-58-7

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C16H18N2O2S

溶于液体

-80℃

六个月

分子量:

302.39

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

60mg/mL (198.41mM)

Ethanol

1.5mg/mL (4.96mM)

Water

Insoluble

体内(现配现用)

 

 

1mg/ml表示微溶或不溶。

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。

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
(Cell-free assay)

200nM

 

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:

 

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:

 

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).

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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摩尔浓度计算公式

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):