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Imidazole Ketone Erastin Sale

(Synonyms: IKE) 目录号 : GC52190

Imidazole Ketone Erastin是一种有效的、代谢稳定的系统xc- 抑制剂和铁凋亡诱导剂。

Imidazole Ketone Erastin Chemical Structure

Cas No.:1801530-11-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,130.00
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2mg
¥780.00
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5mg
¥1,470.00
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25mg
¥4,410.00
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100mg
¥7,280.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

Cell experiment [1]:

Cell lines

DLBCL cells

Preparation Method

DLBCL cells were plated at 10,000 cells per well in white 384-well plates in technical duplicates and incubated overnight. The cells were then treated with 8 µL medium containing a two-fold dilution series of vehicle , Imidazole Ketone Erastin (0.1 nM-100 µM ) with or without Fer-1. After 24 h incubation, 40 µL of 50% Cell Titer-Glo 50% cell culture medium was added to each well and incubated at room temperature with shaking for 15 min.

Reaction Conditions

0.1 nM-100 µM; 24 h

Applications

Imidazole ketone erastin (0.1nM-100µM;24h) potently reduces DLBCL cell number by lipid peroxidation and ferroptosis.

Animal experiment [2]:

Animal models

Male NCG mice

Preparation Method

NCG mice, 6-weeks old, were injected with 10 million SUDHL0-6 cells subcutaneously. The mice were treated after the tumor size reached 100 mm3. Mice were separated randomly into treatment groups and dosed with 23 mg/kg Imidazole Ketone Erastin , 40 mg/kg Imidazole Ketone Erastin , 23 mg/kg Imidazole Ketone Erastin PEG-PLGA nanoparticles , vehicle 1, and vehicle 2 once daily by IP for 14 days.

Dosage form

23, 40 mg/kg/d ; 14 days ; i.p.

Applications

Imidazole Ketone Erastin inhibited tumor growth in a diffuse large B cell lymphoma mouse model, caused a significant decrease in tumor growth and weight loss starting from day 9.

References:

[1] Zhang, Y., Tan, H., Daniels, J.D., et al. Imidazole ketone erastin induces ferroptosis and slows tumor growth in a mouse lymphoma model. Cell Chem. Biol. 26(5), 623-633 (2019).

产品描述

Imidazole Ketone Erastin is an effective and metabolically stable system xc- inhibitor and ferroptosis inducer. Ferroptosis is a regulated form of cell death that can be induced by inhibiting the cystine-glutamate antiporter system xc- [1].

In vitro, Imidazole Ketone Erastin (0.1 nM-100 µM; 24 h) effectively reduces the number of DLBCL cells by inducing lipid peroxidation and ferroptosis, with 18 DLBCL cell lines displaying varying sensitivities to the inhibition by Imidazole Ketone Erastin [1]. Imidazole Ketone Erastin (1-250 nM; 24 h) depletes reduced glutathione in a dose-dependent manner, with an IC50 of 34 nM in SUDHL 6 cells, and also increases lipid ROS [1].

In vivo, Imidazole Ketone Erastin (23, 40 mg/kg/d; i.p.) inhibits tumor growth in a mouse model of diffuse large B cell lymphoma, leading to a significant reduction in tumor growth and body weight loss starting from day 9 [1]. Imidazole Ketone Erastin (40 mg/kg; i.p.) administered every other day for 22 days to mice with a model of chronic arthritis significantly alleviates symptoms of synovitis and promotes the rapid resolution of inflammation [2].

References:
[1]Zhang, Y., Tan, H., Daniels, J.D., et al. Imidazole ketone erastin induces ferroptosis and slows tumor growth in a mouse lymphoma model. Cell Chem. Biol. 26(5), 623-633 (2019).
[2] TNF antagonist sensitizes synovial fibroblasts to ferroptotic cell death in collagen-induced arthritis mouse models[J]. Nature Communications[2024-03-08].

Imidazole Ketone Erastin是一种有效的、代谢稳定的系统xc- 抑制剂和铁凋亡诱导剂。铁凋亡是一种受调节的细胞死亡形式,其可通过抑制胱氨酸-谷氨酸反向转运蛋白系统xc- 而诱导[1]。

在体外,Imidazole Ketone Erastin (0.1 nM-100 µM; 24 h) 通过诱导脂质过氧化和铁凋亡可以有效减少DLBCL细胞数量,18种DLBCL细胞系均显示出对Imidazole Ketone Erastin抑制的不同敏感性[1]。Imidazole Ketone Erastin(1-250 nM; 24 h)以剂量依赖性方式消耗还原型谷胱甘肽,在SUDHL 6细胞中IC50 为34 nM,还增加脂质ROS[1]。

在体内,Imidazole Ketone Erastin (23, 40 mg/kg/d; i.p.) 抑制弥漫性大 B 细胞淋巴瘤小鼠模型中的肿瘤生长,从第9天开始导致肿瘤生长和体重减轻显着减少[1]。Imidazole Ketone Erastin(40 mg/kg; i.p.)每两天一次对慢性关节炎模型小鼠进行治疗,持续22天,显著减轻了滑膜炎症状,促进了炎症的迅速消退[2]。

Chemical Properties

Cas No. 1801530-11-9 SDF Download SDF
别名 IKE
Canonical SMILES O=C1N(C2=CC(C(CN3C=NC=C3)=O)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=CC=CC=C61
分子式 C35H35ClN6O5 分子量 655.1
溶解度 DMF: 10mg/mL; DMSO: 100mg/mL; DMSO:PBS (pH 7.2) (1:2): 0.25mg/mL 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.5265 mL 7.6324 mL 15.2648 mL
5 mM 0.3053 mL 1.5265 mL 3.053 mL
10 mM 0.1526 mL 0.7632 mL 1.5265 mL
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