CMLD012612 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. It inhibits cell translation and is cytotoxic to NIH/3T3 cells (IC50: 2 nM).

The primary mechanism of action of CMLD012612 is dependent on eIF4A1 since eIF4A1em1jp cells are at least 10-fold more resistant than parental NIH/3T3 cells. The sensitivity of eIF4A1em1jp cells to CMLD012612 observed at higher concentrations may be due to the presence of wild-type eIF4A2 in the cells.

When administered to mice bearing myr-Akt/Em-Myc lymphomas, CMLD012612 (0.2 mg/kg; i.p.; daily; for 5 days; female C57BL/6 mice) treatment effectively synergizes with Doxorubicin, leading to complete tumor loss. CMLD012612 (0.5 mg/kg; i.p.; for 3 hours; female C57BL/6 mice) treatment effectively suppresses liver polysomes 3 hours after injection.

2368900-35-8

C31H33N3O7

559.61

CMLD012612

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years