Imidazole Ketone Erastin (Synonyms: IKE)

Cell lines

DLBCL cells

Preparation Method

DLBCL cells were plated at 10,000 cells per well in white 384-well plates in technical duplicates and incubated overnight. The cells were then treated with 8 µL medium containing a two-fold dilution series of vehicle , Imidazole Ketone Erastin (0.1 nM-100 µM ) with or without Fer-1. After 24 h incubation, 40 µL of 50% Cell Titer-Glo 50% cell culture medium was added to each well and incubated at room temperature with shaking for 15 min.

Reaction Conditions

0.1 nM-100 µM; 24 h

Applications

Imidazole ketone erastin (0.1nM-100µM;24h) potently reduces DLBCL cell number by lipid peroxidation and ferroptosis.

Animal models

Male NCG mice

Preparation Method

NCG mice, 6-weeks old, were injected with 10 million SUDHL0-6 cells subcutaneously. The mice were treated after the tumor size reached 100 mm3. Mice were separated randomly into treatment groups and dosed with 23 mg/kg Imidazole Ketone Erastin , 40 mg/kg Imidazole Ketone Erastin , 23 mg/kg Imidazole Ketone Erastin PEG-PLGA nanoparticles , vehicle 1, and vehicle 2 once daily by IP for 14 days.

Dosage form

23, 40 mg/kg/d ; 14 days ; i.p.

Applications

Imidazole Ketone Erastin inhibited tumor growth in a diffuse large B cell lymphoma mouse model, caused a significant decrease in tumor growth and weight loss starting from day 9.

References:

[1] Zhang, Y., Tan, H., Daniels, J.D., et al. Imidazole ketone erastin induces ferroptosis and slows tumor growth in a mouse lymphoma model. Cell Chem. Biol. 26(5), 623-633 (2019).