1. Cell Cycle/DNA Damage Cytoskeleton
  2. Kinesin
  3. Dimethylenastron

Dimethylenastron 是一种有效的驱动蛋白 Eg5 抑制剂,IC50 值为 200 nM。

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Dimethylenastron Chemical Structure

Dimethylenastron Chemical Structure

CAS No. : 863774-58-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770
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1 mg ¥320
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5 mg ¥700
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10 mg ¥1100
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50 mg ¥3000
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100 mg ¥4500
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500 mg   询价  

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dimethylenastron is a potent kinesin Eg5 inhibitor, with an IC50 of 200 nM.

IC50 & Target[1]

Eg5

200 nM (IC50)

体外研究
(In Vitro)

Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM. 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, 1 μM) causes accumulation of cells in G2/M in HeLa cells[1]. Dimethylenastron (3 and 10 μM) concentration-dependently suppresses the migratory ability of the cancer cells in PANC1 pancreatic cancer cells after treatment for 24 h, but does not inhibit the proliferation of cancer cells at 24 h until 72 h. Dimethylenastron also reduces invasion ability of the cancer cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Dimethylenastron (1.0 µmol) induces a milder scarring but the length of bleb survival is not significantly prolonged compared with the control group. Dimethylenastron (1.0 µmol) 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

302.39

Formula

C16H18N2O2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (330.70 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3070 mL 16.5349 mL 33.0699 mL
5 mM 0.6614 mL 3.3070 mL 6.6140 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.27 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.27 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3070 mL 16.5349 mL 33.0699 mL 82.6747 mL
5 mM 0.6614 mL 3.3070 mL 6.6140 mL 16.5349 mL
10 mM 0.3307 mL 1.6535 mL 3.3070 mL 8.2675 mL
15 mM 0.2205 mL 1.1023 mL 2.2047 mL 5.5116 mL
20 mM 0.1653 mL 0.8267 mL 1.6535 mL 4.1337 mL
25 mM 0.1323 mL 0.6614 mL 1.3228 mL 3.3070 mL
30 mM 0.1102 mL 0.5512 mL 1.1023 mL 2.7558 mL
40 mM 0.0827 mL 0.4134 mL 0.8267 mL 2.0669 mL
50 mM 0.0661 mL 0.3307 mL 0.6614 mL 1.6535 mL
60 mM 0.0551 mL 0.2756 mL 0.5512 mL 1.3779 mL
80 mM 0.0413 mL 0.2067 mL 0.4134 mL 1.0334 mL
100 mM 0.0331 mL 0.1653 mL 0.3307 mL 0.8267 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Dimethylenastron
目录号:
HY-19944
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