Tomivosertib hydrochloride
Based on 17 publication(s) in Google Scholar
Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines. Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance.
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- CAS No.: 1849590-02-8
- 화학식: C17H21ClN6O2
- 분자량:376.84
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Tomivosertib hydrochloride
More- Signal Transduct Target Ther. 2026 Jul 20;11(1):281. [Abstract]
- Nat Chem Biol. 2022 Sep;18(9):942-953. [Abstract]
- Brain. 2024 Sep 3;147(9):2991-2997. [Abstract]
- Clin Cancer Res. 2024 Oct 1;30(19):4464-4481. [Abstract]
- Mol Psychiatry. 2026 Mar 7. [Abstract]
- Oncogene. 2021 Mar;40(10):1851-1867. [Abstract]
- J Med Chem. 2026 May 28;69(10):12543-12564. [Abstract]
- PLoS Biol. 2022 Jun 1;20(6):e3001653. [Abstract]
- Front Endocrinol. 2023 May 25:14:1139874. [Abstract]
- J Virol. 2024 Feb 20;98(2):e0194823. [Abstract]
- Neurobiol Pain. 2024 Jul 26:16:100159. [Abstract]
- Animals (Basel). 2026 Jul 18;16(14):2229.
- Vet Microbiol. 2026 Jan:312:110818. [Abstract]
- bioRxiv. 2026 May 21:2026.05.19.726221. [Abstract]
- bioRxiv. 2025 Apr 1:2025.03.26.645611. [Abstract]
- bioRxiv. 2024 Apr 6.
- bioRxiv. 2023 Jun 14:2023.06.13.544811. [Abstract]
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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WB
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Others
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WB
Biological Activity
제품 설명
IC50 & Target
IC50: 1-2 nM (MNK1), 1-2 nM (MNK2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1 nM
Compound: eFT-508
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Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
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[PMID: 30530193] |
| HEK293 | IC50 |
2 nM
Compound: eFT-508
|
Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
|
[PMID: 30530193] |
Chemical Information
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CAS No. 1849590-02-8
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분자량 376.84
-
화학식 C17H21ClN6O2
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SMILES
O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4.Cl
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Synonyms
eFT508 hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (17)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Dual-targeting pharmacological UFMylation inhibition reprograms tumor and immune microenvironments to achieve long-term glioblastoma regression. [Abstract]2026 Jul 20;11(1):281. PMID: 42472853 -
Nat Chem Biol
2022 Sep;18(9):942-953. PMID: 35697798
Tomivosertib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2022 Sep;18(9):942-953. [Abstract]
Immunoblot analysis was performed on PANC-1 cell lysates to detect the expression of phosphorylated eIF4E (Ser 209; p-eIF4E), total eIF4E, and actin. These cells were treated with DMSO, CID661578, cercariaein, CGP57380, or eFT508 (Tomivosertib: 40 μM) for 6 hours.
Tomivosertib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2022 Sep;18(9):942-953. [Abstract]
Six-day-old zebrafish larvae underwent β-cell ablation and were treated with DMSO, CID661578, eFT508, or a combination of CID661578 and eFT508 (Tomivosertib: 10 μM) for 48 hours. The number of β-cells was then quantitatively analyzed.
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Brain
Tomivosertib reduces ectopic activity in dorsal root ganglion neurons from patients with radiculopathy. [Abstract]2024 Sep 3;147(9):2991-2997. PMID: 39046204
Tomivosertib hydrochloride purchased from MedChemExpress. Usage Cited in: Brain. 2024 Sep 3;147(9):2991-2997. [Abstract]
MNK inhibition with eFT508 (Tomivosertib: 25 nM) rapidly decreases phosphorylated eIF4E in human dorsal root ganglion neurons. Representative enlarged images of p-eIF4E immunostaining (red) and neuronal marker, peripherin (blue).
Tomivosertib hydrochloride purchased from MedChemExpress. Usage Cited in: Brain. 2024 Sep 3;147(9):2991-2997. [Abstract]
Treatment with eFT508 (Tomivosertib: 25 nM) reverses spontaneous activity in human dorsal root ganglion neurons associated with painful dermatomes.
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Clin Cancer Res
Pharmacologic inhibition of eIF4A blocks NRF2 synthesis to prevent osteosarcoma metastasis. [Abstract]2024 Oct 1;30(19):4464-4481. PMID: 39078310 -
Mol Psychiatry
Correction of eIF4E overactivation rescues translatome imbalance and core ASD-like behaviors in valproic acid-induced offspring mice. [Abstract]2026 Mar 7. PMID: 41795048 -
Oncogene
2021 Mar;40(10):1851-1867. PMID: 33564073
Tomivosertib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2021 Mar;40(10):1851-1867. [Abstract]
Protein levels of eIF4E and MCL1 in LPS141 and MESSA cells upon treatment with eFT508 (30 μM, 24 h). The result indicates a inhibition of p-4E at 30 μM.
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J Med Chem
2026 May 28;69(10):12543-12564. PMID: 42126237 -
PLoS Biol
RSK1 promotes mammalian axon regeneration by inducing the synthesis of regeneration-related proteins. [Abstract]2022 Jun 1;20(6):e3001653. PMID: 35648763 -
Front Endocrinol
ZIP9 mediates the effects of DHT on learning, memory and hippocampal synaptic plasticity of male Tfm and APP/PS1 mice. [Abstract]2023 May 25:14:1139874. PMID: 37305050 -
J Virol
Phospho-eIF4E stimulation regulates coronavirus entry by selective expression of cell membrane-residential factors. [Abstract]2024 Feb 20;98(2):e0194823. PMID: 38299843 -
Neurobiol Pain
Interleukin-6 induces nascent protein synthesis in human dorsal root ganglion nociceptors primarily via MNK-eIF4E signaling. [Abstract]2024 Jul 26:16:100159. PMID: 39156884 -
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Vet Microbiol
Mechanistic link between eIF4E phosphorylation and viral pathogenesis: Therapeutic insights from a porcine model. [Abstract]2026 Jan:312:110818. PMID: 41418357 -
bioRxiv
Live cell imaging reveals paclitaxel-induced lysosome motility and function disruption in DRG neurons. [Abstract]2026 May 21:2026.05.19.726221. PMID: 42239088 -
bioRxiv
Expansion of OSMR expression and signaling in the human dorsal root ganglion links OSM to neuropathic pain. [Abstract]2025 Apr 1:2025.03.26.645611. PMID: 40236060 -
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bioRxiv
MNK inhibitor eFT508 (Tomivosertib) suppresses ectopic activity in human dorsal root ganglion neurons from dermatomes with radicular neuropathic pain. [Abstract]2023 Jun 14:2023.06.13.544811. PMID: 37398249
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)