货号	规格	价格	上海	北京	珠海	重庆	武汉
S88321-5mg买3赠1	99.90%	￥600.00 S88321-5mg ￥600.00 现货（买3赠1）	5 5	-	-	-	-
S88321-10mg促销	99.90%	￥1000.00 ￥800.00 S88321-10mg ￥800.00 现货	8 8	-	-	-	-
S88321-25mg促销	99.90%	￥1800.00 ￥1440.00 S88321-25mg ￥1440.00 现货	5 5	-	-	-	-
S88321-50mg促销	≥98%	￥3000.00 ￥2400.00 S88321-50mg ￥2400.00 2-3天	0 货期：2-3天	-	-	-	-
S88321-100mg促销	≥98%	￥4800.00 ￥3840.00 S88321-100mg ￥3840.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

E260 is a Fer/FerT kinase inhibitor.

靶点：

Fer/FerT kinase;Fer/FerTkinase

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 (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 charact

体内研究：

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

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.28 ml	11.399 ml	22.798 ml
5 mM	0.456 ml	2.28 ml	4.56 ml
10 mM	0.228 ml	1.14 ml	2.28 ml
50 mM	0.046 ml	0.228 ml	0.456 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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