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Tomivosertib

Catalog No. T3468 CAS 1849590-01-7

Synonyms: eFT508

Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Tomivosertib, CAS 1849590-01-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 59.00
5 mg	In stock	$ 172.00
10 mg	In stock	$ 255.00
25 mg	In stock	$ 478.00
50 mg	In stock	$ 691.00
100 mg	In stock	$ 983.00
1 mL * 10 mM (in DMSO)	In stock	$ 189.00

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Purity: 99.67%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.
Targets&IC50	MNK1:1-2 nM, MNK2:1-2 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[1].
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[1].
Cell Research	TMD8 cells are treated with the indicated concentrations of eFT508 for 24 h. Cell lysates are subjected to m7-GTP Sepharose pull-down and bound proteins are analyzed by immunoblotting with the indicated antibodies. (Only for Reference)

Synonyms	eFT508
Molecular Weight	340.38
Formula	C17H20N6O2
CAS No.	1849590-01-7

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: <1 mg/mL

DMSO: 11 mg/mL (32.3 mM)

Ethanol: <1 mg/mL

References and Literature

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). Abstract#1554. 2. Suarez M, Blyth G T, Mina A A, et al. Inhibitory effects of Tomivosertib in acute myeloid leukemia[J]. Oncotarget. 2021, 12(10): 955.

Citations

1. Suarez M, Blyth G T, Mina A A, et al. Inhibitory effects of Tomivosertib in acute myeloid leukemia. Oncotarget. 2021, 12(10): 955.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Hematonosis Compound Library Bioactive Compound Library Anti-Prostate Cancer Compound Library PPI Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Tomivosertib 1849590-01-7 Apoptosis Cell Cycle/Checkpoint Immunology/Inflammation MAPK PD-1/PD-L1 MNK Inhibitor MAP kinase interacting kinase Mitogen activated protein kinase interacting kinase MAPK interacting kinase eFT 508 eFT-508 eFT508 inhibit inhibitor

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