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CAS No.: 1241537-79-0

E260 Catalog No. CSN24156

E260 is an inhibitor of the Fer/FerT kinase with Kd of 0.85 μM, selectively evokes metabolic stress and necrotic death in cancer cells.

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技术信息

生物活性

描述Disruption of the reprogrammed energy management system of malignant cells is a prioritized goal of targeted cancer therapy. Two regulators of this system are the Fer kinase, and its cancer cell specific variant, FerT, both residing in subcellular compartments including the mitochondrial electron transport chain. E260 is a newly developed inhibitor of Fer and FerT with a Kd of 0.85 µM. Onset of death was 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. Importantly, no death was seen in normal human fibroblasts (Hfb) or normal human epithelial cells, that were treated with E260 under the same conditions. In two other CC cell lines, HCT116 and SW48, which are derived from grade II and grade IV colon carcinoma tumors, respectively, the EC₅₀ values for E260 after 24 h of treatment were above 5 µM. Treatment of the grade IV SW48 cells with 2 µM E260 for 48 h led to their complete death, HCT116 cells treated under these conditions reached only 25% cell death. E260 exhibited an EC₅₀ of 3.2 µM after 72 h treatment of non-metastatic PANC-1 cells. In comparison, SU.86.86 which are metastatic ductal carcinoma cells, proved to be more susceptible to E260 with an EC₅₀ of 1.1 µM after 72 h of treatment. Moreover, a decrease of 35%–40% was observed in the cellular ATP level of CC cells treated with 2 µM E260 for 12 h, a time point preceding the onset of death. In immuno-compromised “Nude” mice introduced with SW620 cells, administration of E260 (25 mg/kg or 50 mg/kg) led 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^[1].
作用机制E260 binds the Fer/FerT C-terminal portion^[1].
参考文献

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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2798 mL
- 11.3991 mL
- 22.7982 mL
- 5 mM
- 0.4560 mL
- 2.2798 mL
- 4.5596 mL
- 10 mM
- 0.2280 mL
- 1.1399 mL
- 2.2798 mL

技术信息

CAS号

1241537-79-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H34N6S

运输

蓝冰

分子量

438.63

别名

溶解度

DMSO	410.0 mg/mL (934.7 mM)
Water	insoluble

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E260 Catalog No. CSN24156

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