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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
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 IC 50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity
In Vitro
The IC 50 of CMLD012612 toward NIH/3T3 cells is 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57BL/6 mice Dosage: 0.5 mg/kg Administration: Intraperitoneal injection; for 3 hours Result: Effectively suppressed liver polysomes 3 hours after injection.
Form:Solid
IC50& Target:eIF4A
| Canonical Smiles | CC1=NC23C4=C(C=C(C=C4OC)OC)OC2(C(C(C3(N1)O)C(=O)N(C)OC)C5=CC=CC=C5)C6=CC=C(C=C6)OC |
|---|---|
| IUPAC Name | (1R,9R,10S,11R,12R)-12-hydroxy-N,3,5-trimethoxy-9-(4-methoxyphenyl)-N,14-dimethyl-10-phenyl-8-oxa-13,15-diazatetracyclo[7.6.0.01,12.02,7]pentadeca-2(7),3,5,14-tetraene-11-carboxamide |
| InChIKey | GEGBQVSIWBLDJE-GRNIXUCMSA-N |
| INCHI | 1S/C31H33N3O7/c1-18-32-30-26-23(39-5)16-22(38-4)17-24(26)41-29(30,20-12-14-21(37-3)15-13-20)25(19-10-8-7-9-11-19)27(31(30,36)33-18)28(35)34(2)40-6/h7-17,25,27,36H,1-6H3,(H,32,33)/t25-,27+,29+,30-,31-/m1/s1 |
| PubChem CID | 145712379 |
| Molecular Weight | 559.61 |
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