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[CAS NO. 1849590-01-7] Tomivosertib
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-100022 |
| Brand: | MCE |
| CAS: | 1849590-01-7 |
Overview
| MDL | MFCD30489732 |
|---|---|
| Molecular Weight | 340.38 |
| Molecular Formula | C17H20N6O2 |
| SMILES | O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4 |
3 Publications Citing Use of MCE
Summary
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC 50 s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC 50 =2-16 nM) in tumor cell lines [1] . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance [2] .
IC50 & Target
|
MNK1 1-2 nM (IC 50 ) |
MNK2 1-2 nM (IC 50 ) |
PD-L1
|
In Vitro
Tomivosertib (eFT508) reduces eIF4E phosphorylation dose-dependently at serine 209 (IC 50 =2-16 nM) in tumor cell lines. In a panel of appr 50 hematological cancers, Tomivosertib shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to Tomivosertib 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 Tomivosertib mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Tomivosertib (eFT508) shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, Tomivosertib combines effectively with components of R-CHOP and with novel targeted agents, including PCI-32765 and Venetoclax, in human lymphoma models [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04261218 | Translational Research in Oncology|Effector Therapeutics|Stand Up To Cancer |
Breast Cancer
|
August 25, 2020 | Phase 1 |
| NCT04622007 | Effector Therapeutics|Medpace, Inc. |
Non-small Cell Lung Cancer
|
June 2, 2021 | Phase 2 |
| NCT02937675 | Effector Therapeutics |
Lymphoma
|
February 8, 2017 | Phase 1|Phase 2 |
| NCT02605083 | Effector Therapeutics |
Cancer
|
December 3, 2015 | Phase 1|Phase 2 |
| NCT03690141 | Effector Therapeutics |
Castrate-resistant Prostate Cancer (CRPC)
|
October 12, 2018 | Phase 2 |
| NCT03318562 | Effector Therapeutics |
Triple Negative Breast Cancer|Hepatocellular Carcinoma
|
November 21, 2017 | Phase 2 |
| NCT03258398 | Effector Therapeutics|Merck KGaA, Darmstadt, Germany|Pfizer |
Microsatellite Stable Relapsed or Refractory Colorectal Cancer
|
September 18, 2017 | Phase 2 |
| NCT03616834 | Effector Therapeutics |
Solid Tumors
|
July 25, 2018 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 4.35 mg/mL ( 12.78 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9379 mL | 14.6895 mL | 29.3789 mL |
| 5 mM | 0.5876 mL | 2.9379 mL | 5.8758 mL |
| 10 mM | 0.2938 mL | 1.4689 mL | 2.9379 mL |
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.
- [2] Xu Y, et al. Translation control of the immune checkpoint in cancer and its therapeutic targeting. Nat Med. 2019 Feb;25(2):301-311.
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