Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Tomivosertib [1849590-01-7]

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Referência NB-64-22464-1mg

Tamanho : 1mg

Marca : Neo Biotech

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Tomivosertib

(Synonyms: eFT508) Copy Product Info

Synonyms: eFT508

Catalog No. T3468 Copy Product Info

Purity: 99.72%

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

Cas No. 1849590-01-7

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.72%

Color:White to Yellow

Product Introduction

Bioactivity

Description	Tomivosertib (eFT508) is a potent and highly selective MNK1 and MNK2 inhibitor with an IC₅₀ value of 1-2 nM.
Targets & IC50	MNK1:1-2 nM, MNK2:1-2 nM
In vitro	Tomivosertib 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 Tomivosertib leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~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[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].
Synonyms	eFT508
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)

Chemical Properties

Molecular Weight	340.38
Formula	C₁₇H₂₀N₆O₂
Cas No.	1849590-01-7
Smiles	Cc1cc(Nc2cc(N)ncn2)c(=O)n2c1C(=O)NC21CCCCC1
Relative Density.	1.43 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: <1 mg/mL

DMSO: 11 mg/mL (32.32 mM), Sonication is recommended.

Ethanol: <1 mg/mL

In Vivo Formulation

10% DMSO+90% Saline: 1.1 mg/mL (3.23 mM), Suspension.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9379 mL	14.6895 mL	29.3789 mL	146.8946 mL
5 mM	0.5876 mL	2.9379 mL	5.8758 mL	29.3789 mL
10 mM	0.2938 mL	1.4689 mL	2.9379 mL	14.6895 mL
20 mM	0.1469 mL	0.7345 mL	1.4689 mL	7.3447 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

TomivosertibPD-L1PDL1PD-1/PD-L1PD1/PDL1PD-1PD1MNK2MNK1MNKMitogen activated protein kinase interacting kinaseMAPK interacting kinaseMAP kinase interacting kinaseInhibitorinhibiteFT-508eFT 508

Related Tags: Tomivosertib chemical structure | Tomivosertib in vivo | Tomivosertib in vitro | Tomivosertib formula | Tomivosertib molecular weight