연구용

Erastin Ferroptosis inducer

제품 번호: S7242

Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions are unstable and should be fresh-prepared.
Erastin Ferroptosis activator Chemical Structure

화학 구조

분자량: 547.04

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품질 관리 (Quality Control)

배치: 순도: 99.89%
99.89

함께 자주 사용되는 제품 Erastin

RSL3

This compound and RSL3 as ferroptosis inducers (FINs), sensitize cancer cells (H460/A549) to ionizing radiation (IR).

Liproxstatin-1

Liproxstatin-1 protects against ferroptosis-inducing agents, such as this compound and RSL3 in a dose-dependent manner.

Ferrostatin-1 (Fer-1)

Ferrostatin-1 promotes reversal of this compound-induced ferroptosis in HT-22/HT-1080 dying cells.

Z-VAD-FMK

This compound and Z-VAD-FMK combination does not block its-induced cell death in HS578T/MDAMB231 cells.

Celastrol (Tripterine)

Combined treatment with it induce cell death at nontoxic concentrations

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
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 Cytotoxic assay 10 μM 12 h Cytotoxicity against human BJeLR cells expressing RAS G12V mutant at 10 uM at 12 hrs by trypan blue staining 22832321
human BJ cells Function assay 4.6 μM 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 BJ cells Function assay 9 μM 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 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 A673 cells Function assay Induction of cell death in human A673 cells, EC50=30 μM. 17568748
human MX2 cells Function assay Induction of cell death in human MX2 cells, EC50=18 μM. 17568748
human HOS cells Function assay Induction of cell death in human HOS cells , EC50=17 μM. 17568748
human Hs925.T cells Function assay Induction of cell death in human Hs925.T 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 EWS502 cells Function assay Induction of cell death in human EWS502 cells, EC50=10 μM. 17568748
human BJ cells Function assay Induction of cell death in TERT expressing human BJ cells, EC50=10 μM. 17568748
human TC71 cells Function assay Induction of cell death in human TC71 cells, EC50=10 μM. 17568748
human U937 cells Function assay Induction of cell death in human U937 cells, EC50=10 μM. 17568748
human SK-N-MC cells Function assay Induction of cell death in human SK-N-MC cells, EC50=10 μM. 17568748
human TC32 cells Function assay Induction of cell death in human TC32 cells 17568748
human U2OS cells Function assay Induction of cell death in human U2OS cells, EC50=6 μM. 17568748
human LNCaP cells Function assay Induction of cell death in human LNCaP cells, EC50=6 μM. 17568748
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 SKUT cells Function assay Induction of cell death in human SKUT cells, EC50=4 μM. 17568748
human MES-SA cells Function assay Induction of cell death in human MES-SA cells, EC50=3 μM. 17568748
human SVR cells Function assay Induction of cell death in human SVR cells, EC50=2.5 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 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 HeLa cells Function assay Induction of cell death in human HeLa cells, EC50=0.6 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
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 547.04 화학식

C30H31ClN4O4

보관 (수령일로부터) 3 years -20°C powder
CAS 번호 571203-78-6 SDF 다운로드 원액 보관 용액은 불안정합니다. 신선하게 준비하거나 소량의 사전 포장된 크기를 구매하십시오. 수령 즉시 재포장하십시오.
동의어 N/A Smiles CCOC1=CC=CC=C1N2C(=O)C3=CC=CC=C3N=C2C(C)N4CCN(CC4)C(=O)COC5=CC=C(C=C5)Cl

용해도 (Solubility)

In vitro
배치:

DMSO : 25 mg/mL (45.7 mM) 50°C 수조에서 가온; 초음파 처리;
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
Ferroptosis
시험관 내(In vitro)

Erastin is selectively lethal to oncogenic RAS-mutant cell lines, and triggers a unique iron-dependent form of non-apoptotic cell death called ferroptosis.

This compound binds directly to VDAC2 and causes mitochondrial damage via ROS production in an NADH-dependent manner, which induces cell death in some tumor cells harbouring activating mutations in the RAS-RAF-MEK pathway.

In addition, this chemical, via inducing ROS-mediated CID (Caspase-independent cell death), strongly enhances the effect in WT EGFR cells.

생체 내(In vivo)

Erastin is a ferroptosis activator by inhibiting voltage-dependent anion channels (VDAC2/VDAC3). This compound also inhibits cystine-glutamate antiporter (xCT).

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/23344263/
  • [5] https://pubmed.ncbi.nlm.nih.gov/35197442/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot GPX4 / cleaved-PARP / cleaved-caspase3 / LC3 / p62 / LDH / HMGB1 TfR1 / p-JNK / JNK / p-P38 HSPA5 / p-EIF2AK3 GRP78
S7242-WB1
27308510
Growth inhibition assay Cell survival
S7242-viability1
29348676
Immunofluorescence HMGB1
S7242-IF1
31105999