Introduction：Basic information about CAS 1849590-01-7|eFT508, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | eFT508 |
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| CAS Number | 1849590-01-7 | Molecular Weight | 340.380 |
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| Density | 1.4±0.1 g/cm3 | Boiling Point | 735.6±60.0 °C at 760 mmHg |
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| Molecular Formula | C17H20N6O2 | Melting Point | / |
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| MSDS | / | Flash Point | 398.7±32.9 °C |
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Names
| Name | 6'-[(6-Amino-4-pyrimidinyl)amino]-8'-methyl-2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione |
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| Synonym | More Synonyms |
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eFT508 BiologicalActivity
| Description | eFT508 is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. |
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| Related Catalog | Signaling Pathways >>MAPK/ERK Pathway >>MNKResearch Areas >>Cancer |
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| Target | MNK1:1-2 nM (IC50) MNK2:1-2 nM (IC50) |
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| In Vitro | eFT508 reduces eIF4E phosphorylation dose-dependently at serine 209 (IC50=2-16 nM) in tumor cell lines. In a panel of appr 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. Further evaluation eFT508 mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life[1]. |
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| In Vivo | eFT508 shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, eFT508 combines effectively with components of R-CHOP and with novel targeted agents, including ibrutinib and venetoclax, in human lymphoma models[1]. |
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| References | [1]. Kevin R. Webster, et al. eFT508, a Potent and Selective Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 Inhibitor, Is Efficacious in Preclinical Models of Diffuse Large B-Cell Lymphoma (DLBCL). Blood 2015 126:1554; |
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Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
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| Boiling Point | 735.6±60.0 °C at 760 mmHg |
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| Molecular Formula | C17H20N6O2 |
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| Molecular Weight | 340.380 |
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| Flash Point | 398.7±32.9 °C |
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| Exact Mass | 340.164764 |
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| LogP | 1.12 |
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| Vapour Pressure | 0.0±2.4 mmHg at 25°C |
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| Index of Refraction | 1.688 |
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| InChIKey | HKTBYUWLRDZAJK-UHFFFAOYSA-N |
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| SMILES | Cc1cc(Nc2cc(N)ncn2)c(=O)n2c1C(=O)NC21CCCCC1 |
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| Storage condition | -20℃ |
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Synonyms
| Spiro[cyclohexane-1,3'(2'H)-imidazo[1,5-a]pyridine]-1',5'-dione, 6'-[(6-amino-4-pyrimidinyl)amino]-8'-methyl- |
| 6'-[(6-Amino-4-pyrimidinyl)amino]-8'-methyl-2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione |
| eFT508 |
