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目录号 : GC34103

E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that 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.

E260 Chemical Structure

Cas No.:1241537-79-0

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5mg
¥2,790.00
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10mg
¥4,384.00
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25mg
¥8,730.00
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50mg
¥13,500.00
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100mg
¥21,920.00
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Sample solution is provided at 25 µL, 10mM.

Description

E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that 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.

[1] Yoav Elkis, et al. Nat Commun. 2017 Oct 16;8(1):940.

实验参考方法

Kinase experiment:

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].

Cell experiment:

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].

Animal experiment:

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].

References:

[1]. Elkis Y, et al. A novel Fer/FerT targeting compound selectively evokes metabolic stress and necrotic death in malignant cells. Nat Commun. 2017 Oct 16;8(1):940.

化学性质

Cas No. 1241537-79-0 SDF
Canonical SMILES CC(C)C1=CC=C(C2=CN3C(SC(N4CCC(CN5CCN(C)CC5)CC4)=N3)=N2)C=C1
分子式 C24H34N6S 分子量 438.63
溶解度 DMSO : 1 mg/mL (2.28 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2798 mL 11.3991 mL 22.7983 mL
5 mM 0.456 mL 2.2798 mL 4.5597 mL
10 mM 0.228 mL 1.1399 mL 2.2798 mL
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