E260|cas:1241537-79-0|西域试剂

E260,99.91%

产品编号：Bellancom-112097| CAS NO：1241537-79-0| 分子式：C₂₄H₃₄N₆S| 分子量：438.63

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货号	价格	库存与货期
Bellancom-112097	￥3100.00	杭州北京（现货）
Bellancom-112097	￥5000.00	杭州北京（现货）
Bellancom-112097	￥9700.00	杭州北京（现货）
Bellancom-112097	￥15000.00	杭州北京（现货）

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E260

产品介绍

E260 是一种 Fer/FerT 激酶抑制剂。

生物活性

E260 is a Fer/FerT kinase inhibitor.

体外研究

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 (K_d) 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 K_d 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.

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

体内研究

E260 suppresses xenografts progression in vivo. The pharmacokinetic (PK) profile of E260 is determined in mice. E260 exhibits a T_1/2 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.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 1 mg/mL (2.28 mM; Need ultrasonic)

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	---	---	---
10 mM	---	---	---

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, 6 months; -20°C, 1 month。-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。

In Vivo:

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

1.

请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 22 mg/mL (50.16 mM); Suspended solution; Need ultrasonic
2.

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); Clear solution

此方案可获得 ≥ 0.1 mg/mL (0.23 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

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); Clear solution

此方案可获得 ≥ 0.1 mg/mL (0.23 mM，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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.1 mg/mL (0.23 mM); Clear solution

此方案可获得 ≥ 0.1 mg/mL (0.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。