Imidazole Ketone Erastin

Imidazole ketone erastin is an inducer of ferroptosis. It inhibits glutamate release in human CCF-STTG1 astrocytoma cells (IC50 = 30 nM), indicating inhibition of the system xc- cystine/glutamate transporter. Imidazole ketone erastin increases production of lipid reactive oxygen species (ROS) in SUDHL6 diffuse large B cell lymphoma (DLBCL) cells in a concentration-dependent manner, as well as reduces glutathione (GSH) levels in these cells (IC50 = 34 nM). It inhibits the growth of HT-1080 fibrosarcoma cells (GI50 = 310 nM) as well as HRASG12V-overexpressing BJeLR cells (IC50 = 3 nM). Imidazole ketone erastin (23 and 40 mg/kg) reduces tumor growth in an SUDHL6 mouse xenograft model.Formal Name: 2-[[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]methyl]-3-[5-[2-(1H-imidazol-1-yl)acetyl]-2-(1-methylethoxy)phenyl]-4(3H)-quinazolinone. CAS Number: 1801530-11-9. Synonyms: IKE. Molecular Formula: C35H35ClN6O5. Formula Weight: 655.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10mg/mL, DMSO: 1mg/mL, DMSO:PBS (pH 7.2) (1:2): 0.25mg/mL. lambdamax: 227, 275 nm. 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. InChi Code: InChI=1S/C35H35ClN6O5/c1-24(2)47-32-12-7-25(31(43)20-40-14-13-37-23-40)19-30(32)42-33(38-29-6-4-3-5-28(29)35(42)45)21-39-15-17-41(18-16-39)34(44)22-46-27-10-8-26(36)9-11-27/h3-14,19,23-24H,15-18,20-22H2,1-2H3. InChi Key: PSPXJPWGVFNGQI-UHFFFAOYSA-N.