eFT-508
EFT-508
CAS: 1849590-01-7
Molecular Formula: C17H20N6O2
eFT-508 - Names and Identifiers
| Name | EFT-508 |
| Synonyms | EFT-508 CS-2450 eFT-508 eFT508 -MNK Tomivosertib eFT-508 (eFT508) Tomivosertib eFT508 6'-[(6-Amino-4-pyrimidinyl)amino]-8'-methylspiro[cyclohexane-1,3'(2'H)-imidazo[1,5-a]pyridine]-1',5'-dione 6'-((6-aminopyrimidin-4-yl)amino)-8'-methyl-1'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'(2'H)-dione |
| CAS | 1849590-01-7 |
eFT-508 - Physico-chemical Properties
| Molecular Formula | C17H20N6O2 |
| Molar Mass | 340.3797 |
| Density | 1.43±0.1 g/cm3(Predicted) |
| Melting Point | >300°C |
| Boling Point | 735.6±60.0 °C(Predicted) |
| Solubility | DMSO: 6 mg/mL (Need ultrasonic) |
| Appearance | Form Solid, color Pale Yellow |
| pKa | 13.77±0.60(Predicted) |
| Storage Condition | Refrigerator, under inert atmosphere |
| Physical and Chemical Properties | Bioactive Tomivosertib (eFT-508) is an effective and selective inhibitor of MNK1/2 with IC50 of 2.4 nM and 1 nM respectively. It can reduce the proliferation of tumor cells and tumor growth. Tomivosertib (eFT-508) inhibited eIF4E phosphorylation and significantly down-regulated PD-L1 protein abundance. |
eFT-508 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.938 ml | 14.689 ml | 29.379 ml |
| 5 mM | 0.588 ml | 2.938 ml | 5.876 ml |
| 10 mM | 0.294 ml | 1.469 ml | 2.938 ml |
| 5 mM | 0.059 ml | 0.294 ml | 0.588 ml |
Last Update：2024-01-02 23:10:35
eFT-508 - Nature
| Solubility | DMSO (Slightly, Heated), Methanol (Very Slightly) |
Last Update：2024-04-10 22:29:15
eFT-508 - Uses and synthesis methods
Target
Target Value
MNK2
(Cell-free assay) 1 nM
MNK1
(Cell-free assay) 2.4 nM
in vitro studies
In enzymatic experiments, the IC50 values of eFT508 for MNK1/2L subtypes are in the range of 1-2 nM, and the inhibition of MNK is a reversible and ATP competitive process. Treatment of cancer cell lines with eFT508 will result in a concentration-dependent decrease in intracellular eIF4E phosphorylation of serine at position 209, with IC50 = 2-16 nM. Among ~ 50 hematological tumors, eFT508 has antiproliferative activity against multiple DLBCL cell lines. The sensitivity of TMD8, OCL-Ly3 and HBL1 DLBCL cells to eFT508 is related to the concentration-dependent decrease of pro-inflammatory factors (such as TNFα, IL-6, IL-10 and CXCL10).
In vivo studies
eFT508 is well tolerated in vivo and is very effective in MyD88-mutant DLBCL models. In TMD8 and HBL-1 ABC-DLBCL models (subcutaneous injection of human lymphoma xenograft model),eFT508 has significant anti-tumor activity.
Last Update：2024-04-09 21:01:54
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