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IKE (Imidazole Ketone Erastin) Ferroptosis inducer

Cat.No.S8877

IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.
IKE (Imidazole Ketone Erastin) Ferroptosis inducer Chemical Structure

Chemical Structure

Molecular Weight: 655.14

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BJeLR Growth inhibition assay 48 hrs Growth inhibition of human RAS-G12V overexpressing BJeLR cells after 48 hrs by alamar blue assay, IC50 = 0.003 μM. 26231156
CCF-STTG1 Function assay 2 hrs Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry, IC50 = 0.03 μM. 26231156
HT1080 Growth inhibition assay 48 hrs Growth inhibition of human HT1080 cells after 48 hrs by alamar blue assay, GI50 = 0.314 μM. 26231156
DRD Growth inhibition assay 48 hrs Growth inhibition of human RAS-G12V overexpressing DRD cells after 48 hrs by alamar blue assay 26231156
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 655.14 Formula

C35H35ClN6O5

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1801530-11-9 -- Storage of Stock Solutions

Synonyms PUN30119 Smiles CC(C)OC1=C(C=C(C=C1)C(=O)CN2C=CN=C2)N3C(=NC4=CC=CC=C4C3=O)CN5CCN(CC5)C(=O)COC6=CC=C(C=C6)Cl

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (152.63 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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%
% Tween 80
% ddH2O
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Ferroptosis [1]
system xc– [1]
In vitro

Imidazole ketone erastin (IKE) is an erastin analog with nanomolar potency, high metabolic stability, and intermediate water solubility. Its treatment potently reduces DLBCL cell number[1].

References

Applications

Methods Biomarkers Images PMID
Growth inhibition assay Cell viability S8877-viability1 30799221

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01555008 Completed
Type 2 Diabetes Mellitus|Renal Impairment
Lexicon Pharmaceuticals
March 2012 Phase 1
NCT04545450 Completed
Transgenderism|Hypogonadism
Unita Complessa di Ostetricia e Ginecologia
November 4 2008 Phase 3

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