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Moligand™, ≥97% Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
Tomivosertib (eFT-508) Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.
Targets
MNK2 (Cell-free assay); MNK1 (Cell-free assay) 1 nM; 2.4 nM
In vitro
eFT508 has a half-maximal inhibitory concentration (IC50) of 1-2 nM against both MNK isoforms in enzyme assays and inhibits the kinase through a reversible, ATP-competitive mechanism of action. Treatment of tumor cell lines with eFT508 leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, eFT508 shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to eFT508 in TMD8, OCI-Ly3 and HBL1 DLBCL cell lines is associated with dose-dependent decreases in production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10.
In vivo
eFT508 is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of eFT508 is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations.
Cell Research(from reference)
Cell lines:TMD8 cells
Concentrations:0.01, 0.1, 1, 3, 10 μM
Incubation Time:24 h
| ALogP | 1.3 |
|---|
| Pubchem Sid | 504772874 |
|---|---|
| Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/504772874 |
| Sonrisas canónicas | CC1=C2C(=O)NC3(N2C(=O)C(=C1)NC4=NC=NC(=C4)N)CCCCC3 |
| IUPAC Name | 6-[(6-aminopyrimidin-4-yl)amino]-8-methylspiro[2H-imidazo[1,5-a]pyridine-3,1'-cyclohexane]-1,5-dione |
| InChIKey | HKTBYUWLRDZAJK-UHFFFAOYSA-N |
| INCHI | 1S/C17H20N6O2/c1-10-7-11(21-13-8-12(18)19-9-20-13)16(25)23-14(10)15(24)22-17(23)5-3-2-4-6-17/h7-9H,2-6H2,1H3,(H,22,24)(H3,18,19,20,21) |
| Isómeros SMILES | CC1=C2C(=O)NC3(N2C(=O)C(=C1)NC4=NC=NC(=C4)N)CCCCC3 |
| CAS alternativo | 1849590-01-7 |
| PubChem CID | 118598754 |
| Términos de entrada MeSH | 6'-((6-Amino-4-pyrimidinyl)amino)-8'-methyl-2'H-spiro(cyclohexane-1,3'-imidazo(1,5-a)pyridine)-1',5'-dione;eFT508;spiro(cyclohexane-1,3'(2'H)-imidazo(1,5-a)pyridine)-1',5'-dione, 6'-((6-amino-4-pyrimidinyl)amino)-8'-methyl-;tomivosertib |
| Peso molecular | 340.38 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organic acids and derivatives |
| Clase | Carboxylic acids and derivatives |
| Subclass | Carboxylic acid derivatives |
| Intermediate Tree Nodes | Carboxylic acid amides |
| Direct Parent | 2-heteroaryl carboxamides |
| Alternative Parents | Pyridinones Methylpyridines Aminopyrimidines and derivatives Aminopyridines and derivatives Imidolactams Heteroaromatic compounds Secondary carboxylic acid amides Lactams Amino acids and derivatives Secondary amines Azacyclic compounds Primary amines Organopnictogen compounds Organooxygen compounds Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | 2-heteroaryl carboxamide - Methylpyridine - Pyridinone - Aminopyrimidine - Aminopyridine - Imidolactam - Pyrimidine - Pyridine - Heteroaromatic compound - Secondary carboxylic acid amide - Lactam - Amino acid or derivatives - Azacycle - Organoheterocyclic compound - Secondary amine - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Primary amine - Organooxygen compound - Organonitrogen compound - Amine - Aromatic heteropolycyclic compound |
| Descripción | This compound belongs to the class of organic compounds known as 2-heteroaryl carboxamides. These are compounds containing a heteroaromatic ring that carries a carboxamide group. |
| External Descriptors | Not available |
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Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Fecha | Articulo |
|---|---|---|---|
| Certificate of Analysis | Dec 12, 2025 | T413958 | |
| Certificate of Analysis | Dec 12, 2025 | T413958 | |
| Certificate of Analysis | Dec 12, 2025 | T413958 | |
| Certificate of Analysis | Dec 12, 2025 | T413958 | |
| Certificate of Analysis | Dec 12, 2025 | T413958 | |
| Certificate of Analysis | Dec 12, 2025 | T413958 | |
| Certificate of Analysis | Dec 12, 2025 | T413958 | |
| Certificate of Analysis | Sep 24, 2022 | T413958 |
| Solubilidad | Solubility (25°C) In vitro DMSO: 13 mg/mL (38.19 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| Peso molecular | 340.400 g/mol |
| XLogP3 | 1.300 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 2 |
| Exact Mass | 340.165 Da |
| Monoisotopic Mass | 340.165 Da |
| Topological Polar Surface Area | 113.000 Ų |
| Heavy Atom Count | 25 |
| Formal Charge | 0 |
| Complexity | 664.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
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