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CAS No.: 571203-78-6

Erastin/爱拉斯汀 Catalog No. CSN17148

Synonyms: Erastin

Erastin is a compound that interacts with VDAC, blocks and reverses mitochondrial depolarization after microtubule destabilizers in intact cells and antagonized tubulin-induced VDAC blockage in planar bilayers. It is also a ferroptosis inducer.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Erastin is a both Ferroptosis activator and mitochondrial VDAC modulator. Erastin can trigger ferroptosis dependent upon intracellular iron. Treatment with 10μM Erastin for 6h can induce accumulation of cytosolic ROS which can be inhibited by 100μM deferoxamine in HT-1080 cells. Iron-dependent oxidative death and inhibition of System x^-_c can also be observed. Erastin can induce rapid, oxidative, non-apoptotic death in HRAS^V12-expressing cell lines at concentration below 1μM. This lethal effect of erastin is dependent on the RAS–RAF–MEK pathway for inhibition of MAPK, ERK1/ 2 or MEK1/2, or KRAS and BRAF knockdown could restore the lethality of erastin. This selectivity for cells with activated RAS–RAF–MEK signaling may due to the interaction of Erastin with VDAC proteins and the subsequent induction of mitochondrial dysfunction, release of oxidative species and, ultimately, non-apoptotic, oxidative cell death.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human A673 cells	-	Function assay	-	Induction of cell death in human A673 cells, EC50=30 μM.	17568748
human BJ cells	-	Function assay	-	Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of PD-98059 by trypan blue exclusion method, IC50=0.9 μM.	17568748
human BJ cells	-	Function assay	-	Induction of cell death in TERT expressing human BJ cells, EC50=10 μM.	17568748

更多
动物研究
剂量
Mice: 20 mg/kg^[2] (i.v.); 10 mg/kg, 30 mg/kg^[3] (i.p.), 40 mg/kg^[4] (i.p.)

给药途径
i.v., i.p.

动物研究
剂量	Mice: 20 mg/kg^[2] (i.v.); 10 mg/kg, 30 mg/kg^[3] (i.p.), 40 mg/kg^[4] (i.p.)
给药途径	i.v., i.p.

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
- 1.8280 mL
- 9.1400 mL
- 18.2800 mL
- 5 mM
- 0.3656 mL
- 1.8280 mL
- 3.6560 mL
- 10 mM
- 0.1828 mL
- 0.9140 mL
- 1.8280 mL

技术信息

CAS号

571203-78-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H31ClN4O4

运输

蓝冰

分子量

547.04

别名

Erastin

溶解度

DMSO	18.0 mg/mL (32.9 mM)
Water	insoluble

动物实验配方

5%DMSO+40%PEG 300+5%Tween80+water

1.75 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

human A673 cells	-	Function assay	-	Induction of cell death in human A673 cells, EC50=30 μM.	17568748
human BJ cells	-	Function assay	-	Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of PD-98059 by trypan blue exclusion method, IC50=0.9 μM.	17568748
human BJ cells	-	Function assay	-	Induction of cell death in TERT expressing human BJ cells, EC50=10 μM.	17568748
human BJ cells	-	Function assay	-	Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes in presence of U0126 by trypan blue exclusion method, IC50=31.2 μM.	17568748
human BJ cells	9 μM	Function assay	-	Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells at 9 uM.	17568748
human BJ cells	4.6 μM	Function assay	-	Increase in intracellular oxidative species in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells at 4.6 uM	17568748
human BJeH cells	-	Function assay	6 h	Induction of reactive oxygen species production in human BJeH cells expressing wild type RAS after 6 hrs by DCF-based flow cytometric analysis	22832321
human BJeLR cells	10 μM	Cytotoxic assay	12 h	Cytotoxicity against human BJeLR cells expressing RAS G12V mutant at 10 uM at 12 hrs by trypan blue staining	22832321
human Calu1 cells	-	Function assay	-	Inhibition of human Calu1 cells expressing KRAS with activating mutations by trypan blue exclusion assay, IC50=4 μM.	17568748
human CCF-STTG1 cells	-	Function assay	-	Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry, IC50=0.2 μM.	26231156
human EWS502 cells	-	Function assay	-	Induction of cell death in human EWS502 cells, EC50=10 μM.	17568748
human HeLa cells	-	Function assay	-	Induction of cell death in human HeLa cells, EC50=0.6 μM.	17568748
human HOS cells	-	Function assay	-	Induction of cell death in human HOS cells , EC50=17 μM.	17568748
human Hs51.T cells	-	Function assay	-	Induction of cell death in human Hs51.T cells, EC50=12 μM.	17568748
human Hs925.T cells	-	Function assay	-	Induction of cell death in human Hs925.T cells, EC50=17 μM.	17568748
human HT1080 cells	-	Function assay	-	Induction of cell death in human HT1080 cells in presence of PD-98059 by trypan blue exclusion method, IC50=1 μM.	17568748
human LNCaP cells	-	Function assay	-	Induction of cell death in human LNCaP cells, EC50=6 μM.	17568748
human MES-SA cells	-	Function assay	-	Induction of cell death in human MES-SA cells, EC50=3 μM.	17568748
human MX2 cells	-	Function assay	-	Induction of cell death in human MX2 cells, EC50=18 μM.	17568748
human SK-N-MC cells	-	Function assay	-	Induction of cell death in human SK-N-MC cells, EC50=10 μM.	17568748
human SKUT cells	-	Function assay	-	Induction of cell death in human SKUT cells, EC50=4 μM.	17568748
human SVR cells	-	Function assay	-	Induction of cell death in human SVR cells, EC50=2.5 μM.	17568748
human TC32 cells	-	Function assay	-	Induction of cell death in human TC32 cells	17568748
human TC71 cells	-	Function assay	-	Induction of cell death in human TC71 cells, EC50=10 μM.	17568748
human U2OS cells	-	Function assay	-	Induction of cell death in human U2OS cells, EC50=6 μM.	17568748
human U937 cells	-	Function assay	-	Induction of cell death in human U937 cells, EC50=10 μM.	17568748

Erastin/爱拉斯汀 Catalog No. CSN17148

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