Erastin

For research use only. Not for use in humans.

目录号:S7242

Erastin Chemical Structure

CAS No. 571203-78-6

Erastin是一种ferroptosis激活剂,通过作用于线粒体VDAC而起作用,选择性作用于携带致癌基因RAS的肿瘤细胞。

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产品安全说明书

Ferroptosis抑制剂选择性比较

生物活性

产品描述 Erastin是一种ferroptosis激活剂,通过作用于线粒体VDAC而起作用,选择性作用于携带致癌基因RAS的肿瘤细胞。
靶点
Ferroptosis [1]
体外研究

Erastin选择性致死致癌的Ras突变体细胞系,并触发独特的fe依赖性的称为ferroptosis的非凋亡细胞死亡。[1] [2] Erastin直接结合VDAC2并且使得通过NADH-依赖方式产生ROS导致线粒体损害,在一些表达激活突变的肿瘤细胞中,通过RAS-RAF-MEK途径诱导细胞死亡。[3] 此外,erastin通过诱导ROS介导的CID(胱天蛋白酶非依赖性细胞死亡),强烈增强了野生型EGFR细胞的作用。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CCF-STTG1 cells MojLSpVv[3Srb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKFildDDpckBpfW2jbjDDR2YuW1SWR{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[4x2fGGvYYTlJJJmdGWjc3WgZYZ1\XJiMjDodpMh[nliZnz1c5JwdWW2comsJGlEPTB;MD6yJO69VS5? MXmyOlI{OTF3Nh?=
human HeLa cells M4jMbmZ2dmO2aX;uJIF{e2G7 MV;JcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCKZVzhJINmdGy|LDDFR|UxRTBwNjFOwG0v MWOxO|U3QDd2OB?=
human BJ cells Mk\tSpVv[3Srb36gZZN{[Xl? NGjuTVBKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDCTkBk\WyuczDlfJBz\XO|aX7nJHRGWlRuIFzUMEBUXCCjbnSgVmFUKEdzMm[gcZV1[W62IHflcoV{KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIGDEMVk5ODV7IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCvZYToc4QtKEmFNUC9NE46KM7:TT6= MoHxNVc2Pjh5NEi=
human HT1080 cells Mne2SpVv[3Srb36gZZN{[Xl? NHq2VFlKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDIWFExQDBiY3XscJMhcW5icILld4Vv[2Vib3[gVGQuQThyNUmgZpkhfHK7cHHuJIJtfWViZYjjcJV{cW:wIH3leIhw\CxiSVO1NF0yKM7:TT6= NVTiVodiOTd3Nki3OFg>
human SVR cells MYjGeY5kfGmxbjDhd5NigQ>? NYL6b|BzUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gV3ZTKGOnbHzzMEBGSzVyPUKuOUDPxE1w MX2xO|U3QDd2OB?=
human MES-SA cells M1HWOGZ2dmO2aX;uJIF{e2G7 NIfiXoRKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDNSXMuW0FiY3XscJMtKEWFNUC9N{DPxE1w NG\wco0yPzV4OEe0PC=>
human SKUT cells MVjGeY5kfGmxbjDhd5NigQ>? NEP0R3RKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDTT3VVKGOnbHzzMEBGSzVyPUSg{txONg>? NHP1Ro0yPzV4OEe0PC=>
human Calu1 cells M2rs[GZ2dmO2aX;uJIF{e2G7 NYr5VJFIUW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1NUBk\WyuczDlfJBz\XO|aX7nJGtTSVNid3n0bEBi[3SrdnH0bY5oKG23dHH0bY9veyCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44h[XO|YYmsJGlEPTB;NDFOwG0v NWXkNFAxOTd3Nki3OFg>
human LNCaP cells NYjOT2RkTnWwY4Tpc44h[XO|YYm= MXnJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCOTlPhVEBk\WyuczygSWM2OD14IN88UU4> MlvQNVc2Pjh5NEi=
human U2OS cells NVzrUZRpTnWwY4Tpc44h[XO|YYm= NGHIVo9KdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDVNm9UKGOnbHzzMEBGSzVyPU[g{txONg>? MoW5NVc2Pjh5NEi=
human TC32 cells M3jn[GZ2dmO2aX;uJIF{e2G7 NH3VO3NKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDUR|MzKGOnbHzz MUWxO|U3QDd2OB?=
human SK-N-MC cells MkXYSpVv[3Srb36gZZN{[Xl? NEXvOmRKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDTT{1PNU2FIHPlcIx{NCCHQ{WwQVExKM7:TT6= M3XJfFE4PTZ6N{S4
human U937 cells MY\GeY5kfGmxbjDhd5NigQ>? MkO1TY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVUmzO{Bk\WyuczygSWM2OD1zMDFOwG0v M3fj[VE4PTZ6N{S4
human TC71 cells Mnf4SpVv[3Srb36gZZN{[Xl? MXzJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCWQ{exJINmdGy|LDDFR|UxRTFyIN88UU4> NGXLbJAyPzV4OEe0PC=>
human BJ cells MXjGeY5kfGmxbjDhd5NigQ>? NFPFOZBKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBVTVKWIHX4dJJme3OrbnegbJVu[W5iQlqgZ4VtdHNuIFXDOVA:OTBizszNMi=> MojKNVc2Pjh5NEi=
human EWS502 cells M4\hVWZ2dmO2aX;uJIF{e2G7 MoL6TY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iRWfTOVAzKGOnbHzzMEBGSzVyPUGwJO69VS5? Ml7qNVc2Pjh5NEi=
human Hs51.T cells NH7OZWpHfW6ldHnvckBie3OjeR?= Ml7STY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iSIO1NU5VKGOnbHzzMEBGSzVyPUGyJO69VS5? NWS2VlhEOTd3Nki3OFg>
human Hs925.T cells NGjPSItHfW6ldHnvckBie3OjeR?= NYjUNnRFUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gTJM6OjVwVDDj[YxteyxiRVO1NF0yPyEQvF2u NUnpNpl5OTd3Nki3OFg>
human HOS cells NVPBSGl4TnWwY4Tpc44h[XO|YYm= MmflTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iSF;TJINmdGy|IDygSWM2OD1zNzFOwG0v M4LreVE4PTZ6N{S4
human MX2 cells MnLPSpVv[3Srb36gZZN{[Xl? NVjIWIt2UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gUXgzKGOnbHzzMEBGSzVyPUG4JO69VS5? NVv2[JF7OTd3Nki3OFg>
human A673 cells MYjGeY5kfGmxbjDhd5NigQ>? NGjITmNKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDBOlc{KGOnbHzzMEBGSzVyPUOwJO69VS5? MVmxO|U3QDd2OB?=
human BJ cells MornSpVv[3Srb36gZZN{[Xl? M4TlWmlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFLKJINmdGy|IHX4dJJme3OrbnegWGVTXCxiTGSsJHNVKGGwZDDSRXMhTzF{VjDteZRidnRiZ3Xu[ZMhcW5icILld4Vv[2Vib3[gWVAyOjZiYomgeJJ6eGGwIHLseYUh\XilbIXzbY9vKG2ndHjv[EwhUUN3ME2zNU4zKM7:TT6= MoezNVc2Pjh5NEi=
human BJ cells NX\leYRWTnWwY4Tpc44h[XO|YYm= Mnj4PUDPxE1? M37UO2lv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFLKJINmdGy|IHX4dJJme3OrbnegWGVTXCxiTGSsJHNVKGGwZDDSRXMhTzF{VjDteZRidnRiZ3Xu[ZMh[2WubIOgZZQhQSC3TT6= MUmxO|U3QDd2OB?=
human BJ cells NHnTelBHfW6ldHnvckBie3OjeR?= M4TIe|QvPiEQvF2= MkT0TY5kemWjc3WgbY4hcW62cnHj[YxtfWyjcjDvfIll[XSrdnWgd5Bm[2mnczDpckBpfW2jbjDCTkBk\WyuczDlfJBz\XO|aX7nJHRGWlRuIFzUMEBUXCCjbnSgVmFUKEdzMm[gcZV1[W62IHflcoV{KGOnbHzzJIF1KDRwNjD1US=> MXixO|U3QDd2OB?=
human BJeLR cells MVTDfZRwfG:6aXRCpIF{e2G7 NXLIfXBrOTBizszN MUWxNkBp M3nRe2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJL\UyUIHPlcIx{KGW6cILld5NqdmdiUlHTJGcyOlZibYX0ZY51KGG2IEGwJJVOKGG2IEGyJIhzeyCkeTD0dplx[W5iYnz1[UB{fGGrbnnu[y=> NH7INZYzOjh|MkOyNS=>
human BJeH cells NIjLUlBHfW6ldHnvckBie3OjeR?= NF;5bZg3KGh? NFTRO5lKdmS3Y4Tpc44hd2ZicnXhZ5RqfmVib4j5[4VvKHOyZXPp[ZMheHKxZIXjeIlwdiCrbjDoeY1idiCESnXIJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJHJCWyCjZoTldkA3KGi{czDifUBFS0ZvYnHz[YQh\myxdzDjfZRwdWW2cnnjJIFv[Wy7c3nz MkfKNlI5OzJ|MkG=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
GPX4 / cleaved-PARP / cleaved-caspase3 / LC3 / p62 / LDH / HMGB1; 

PubMed: 27308510     


HL-60 and Jurkat cells were treated with erastin (5 μM) for 24 h and subjected to western blot analysis of the indicated proteins in whole cell extracts or supernatant. 

TfR1 / p-JNK / JNK / p-P38; 

PubMed: 31105999     


HL-60/NRAS (Q61L) cells were treated with erastin (5 μM) combined with SP600125 (10 μM) and SB202190 (10 μM) for 48 h. TfR1 expression and the phosphorylation of p38 (p-P38) and JNK1/2 (p-JNK1/2) were assayed by western blot. 

HSPA5 / p-EIF2AK3; 

PubMed: 28130223     


Western blot analysis indicated protein expression in PDAC cells following treatment with erastin (2.5-40 μM) for 24 hours (n=3, *p < 0.05 versus untreated group). 

GRP78; 

PubMed: 29383150     


Cells were treated with 50 μM erastin for various time(1-24 h). Whole-cell extracts were analyzed with immunoblotting assay.

27308510 31105999 28130223 29383150
Growth inhibition assay
Cell survival; 

PubMed: 29348676     


The A375 and G-361 human melanoma cells were treated with erastin (2.5-40 µM) or RSL3 (0.1-10 µM) with or without a cell death inhibitor (ferrostatin-1, 1 µM; ZVAD-FMK, 10 µM; necrosulfonamide, 0.5 µM) for 24 h. Cell death was assayed using a CCK-8 kit. Data shown represent mean ± SD from three independent experiments. ****p < 0.0001.

29348676
Immunofluorescence
HMGB1; 

PubMed: 31105999     


HL-60/NRAS (Q61L) cells were treated with erastin (5 μM) with or without Fer-1 (1 μM) pretreatment for 48 h, and then the nuclear/cytosolic HMGB1 expression was assayed by immunofluorescence(Green, HMGB1; blue, nucleus). 

31105999

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: BJ-TERT/LT/ST/RASV12细胞
  • Concentrations: 5 or 10 μg/mL
  • Incubation Time: 6-11小时
  • Method: BJ-TERT/LT/ST/RASV12细胞接种在100 mm平皿中,并使其生长过夜。细胞用erastin(5或10微克/毫升)处理6,8,或11小时。camptothecin处理(0.4微克/毫升)的对照被维持,在接种的时候处理20小时。处理后,细胞用胰蛋白酶/EDTA孵育并用含血清的新鲜培养基洗1次,然后用磷酸盐缓冲盐水洗涤两次。细胞同1×结合缓冲液重悬。100 μL重悬细胞在5μL的膜联蛋白V-FITC和碘化丙啶iodiode在黑暗中孵育15分钟。然后加入400 μl的1×结合缓冲液S并用流式细胞仪分析。采集数据,并使用CellQuest软件进行分析。只有不被碘化丙啶染色的活细胞使用FL1通道的膜联蛋白V-FITC染色分析。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 19 mg/mL (34.73 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5%DMSO+40%PEG 300+5%Tween80+ddH2O
1.75mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 547.04
化学式

C30H31ClN4O4

CAS号 571203-78-6
储存条件 3年 -20°C 粉状
1个月 -80°C 溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID