| Chemical Properties | Back Directory | [Boiling point ]
721.6±70.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
12.37±0.70(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity[1]. | [in vivo]
CMLD012612 (0.5 mg/kg; intraperitoneal injection; for 3 hours; female C57BL/6 mice) treatment effectively suppresses liver polysomes 3 hours after injection, indicating inhibitory activity toward protein synthesis[1].
When administered to mice bearing myr-Akt/Em-Myc lymphomas, CMLD012612 (0.2 mg/kg; intraperitoneal injection; daily; for 5 days; female C57BL/6 mice) treatment effectively synergizes with Doxorubicin, leading to complete tumor loss[1]. | Animal Model: | Female C57BL/6 mice[1] | | Dosage: | 0.5 mg/kg | | Administration: | Intraperitoneal injection; for 3 hours | | Result: | Effectively suppressed liver polysomes 3 hours after injection.
|
| [IC 50]
eIF4 | [References]
[1] Chu J, et al. Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors. Cell Chem Biol. 2019 Nov 21;26(11):1586-1593. DOI:10.1016/j.chembiol.2019.08.008 |
|
|