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E260 是一种 Fer/FerT 激酶抑制剂。

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E260 Chemical Structure

E260 Chemical Structure

CAS No. : 1241537-79-0

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E260 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

E260 is a Fer/FerT kinase inhibitor.

IC50 & Target

Fer/FerT kinase[1]
体外研究
(In Vitro)

E260 is a Fer and FerT inhibitor, which selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. To demonstrate that E260 directly targets Fer and FerT, an in vitro kinase assay is performed using a purified kinase domain (KD)-containing fragment of these enzymes. This analysis demonstrates the direct inhibitory effect of E260 on this domain as reflected by the significantly decreased auto-phosphorylation level of the Fer/FerT KD when incubated with ATP and increasing concentrations of E260. Moreover, computational analysis of E260 docking in the modeled whole Fer protein reveals that the highest scored binding mode of E260 to Fer falls in the ATP-binding pocket of the enzyme’s KD. To measure the dissociation constant (Kd) of E260 from Fer/FerT KD, a microscale thermophoresis (MST) test is performed using ascending concentrations of E260. This analysis corroborates the direct binding of E260 to Fer/FerT KD and determines a Kd of 0.85 µM. To examine the effect of the E260 micellar formulation on Fer in malignant cells, the kinase is immunoprecipitated from untreated and from E260-treated SW620 CC cells. When applied to metastatic grade IV SW620 CC cells, which are serum starved for 16 h and treated with 3 mM H2O2 to activate Fer, E260 exhibits inhibitory effects on the Fer-kinase activity as is reflected by suppressed auto-phosphorylation activity of the enzyme. To characterize the effect of E260 on malignant cells, metastatic SW620 cells are treated with E260 followed by analysis of viability. Onset of death is observed in the E260-treated cells, with an EC50 value of 400 nM after 24 h of treatment and an EC50 of 300 nM after 48 h. E260 exhibits an EC50 of 3.2 µM after 72 h treatment of non-metastatic PANC-1 cells, which are derived from a primary pancreatic ductal carcinoma. Moreover, the maximum death level of these cells after 72 h of treatment with E260 is about 70% following treatment with 4 µM E260. In comparison, SU.86.86 which are metastatic ductal carcinoma cells, prove to be more susceptible to E260 with an EC50 of 1.1 µM after 72 h of treatment and 100% death level imposed by 2 µM E260[1].

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

E260 相关抗体:
体内研究
(In Vivo)

E260 suppresses xenografts progression in vivo. The pharmacokinetic (PK) profile of E260 is determined in mice. E260 exhibits a T1/2 of 175 min in the blood, and a volume of distribution of 4244 mL/kg suggesting an efficient distribution of the compound in the animal tissues. To evaluate the efficacy of E260 on tumor growth, SW620 cells are subcutaneously introduced into immuno-compromised “Nude” mice. Administration of E260 leads to a significant attenuation of tumor progression throughout the experiment, and to a 10-fold decrease in average tumor volume after 22 days of treatment. To further demonstrate the anti-cancer activity of E260 in vivo, mice bearing SW48 cells derived xenografts are treated with E260 and the tumor progression profiles are determined. Mice treated with E260 demonstrate a 5-6-fold attenuation in tumors progression when compared to the control treated group[1].

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

438.63

Formula

C24H34N6S
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 : 1 mg/mL (2.28 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 2.2798 mL 11.3991 mL 22.7983 mL
5 mM --- --- ---
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: ≥ 0.1 mg/mL (0.23 mM); 澄清溶液

    此方案可获得 ≥ 0.1 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 1.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.1 mg/mL (0.23 mM); 澄清溶液

    此方案可获得 ≥ 0.1 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 1.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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： 0.5% CMC-Na/saline water

    Solubility: 22 mg/mL (50.16 mM); 悬浊液; 超声助溶

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

只
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
Kinase Assay
[1]

To test the effect of E260 on the Fer/FerT KD auto-phosphorylation activity, 0.5 µg of the Fer/FerT KD protein is incubated in 0.5 mL kinase activity buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% Brij-35) and 1 µM ATP. As a negative control, the KD protein is incubated in the same buffer without ATP. The KD and ATP containing mixture is incubated for 1 h at room temperature with ascending concentrations of E260 dissolved in DMSO or with DMSO alone. Following the incubation period, a sample from the incubated mixture is separated by SDS-PAGE and a WB analysis is performed using specific anti-Fer and anti-pY antibodies to evaluate the inhibitory effect of E260, as reflected by the diminished phosphorylation level of the Fer/FerT KD[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells death level is determined using the MultiTox-Fluor Multiplex Cytotoxicity Assay. Briefly, SW620 CC cells are inoculated into black 96-well plate. After 24 h, when the cells are completely attached, 2 μM E260 or control solution are administrated at different concentrations and incubated for the desired period of time. Following the incubation period, the assay’s fluorophore which ias used to determine the cell death levels is added to each well. The relative fluorescence intensity emitted by the fluorophore from each well is determined using an ELISA reader and is compared to the florescence intensity obtained from the standard curve drawn to translate it to cell death percentage and normalized to the non-treated cells which are also used in each analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Nude mice are inoculated with 1.5 ×106 SW620 or SW48 CC cells and divided randomly into experimental groups. The mice are transferred from ad libitum diet to a stricter diet 2 days before inoculation to lower blood glucose levels. At this point the mice are also housed one per cage to ensure an even consumption of food. The diet is comprised of 3 g/mouse/day of standard chow, given at the same time every day. The food is consumed within an average time of 2 h, consequently the mice are kept without food for the next 22 h until the daily ration. The mice are kept on this diet throughout the experiment. The mice are randomized 4 days after tumor inoculation and placed again each in a cage. Mice are injected intraperitoneally every 12 h for 22 days with 25 or 50 mg/kg of the micellar E260 formulation, and control mice are injected with empty micelles[1].

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

E260 相关分类

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 2.2798 mL 11.3991 mL 22.7983 mL 56.9956 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.

Keywords:

E2601241537-79-0E 260E-260OthersInhibitorinhibitorinhibit

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