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evobrutinib

Name: evobrutinib
Brand: TargetMol
SKU: T4387
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4387Cas No. 1415823-73-2

Alias MSC2364447C, M2951

Evobrutinib(M2951) , also known as M-2951 and MSC-2364447C, is a highly selective inhibitor of the Bruton's tyrosine kinase (BTK), which is important in the development and functioning of various immune cells including B -lymphocytes and macrophages. PreClinical research suggests it may be therapeutically useful in certain autoimmune diseases.

evobrutinib

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Purity: 99.58%

Catalog No. T4387Alias MSC2364447C, M2951Cas No. 1415823-73-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$35	In Stock	In Stock
5 mg	$81	In Stock	In Stock
10 mg	$129	In Stock	In Stock
25 mg	$239	In Stock	In Stock
50 mg	$347	In Stock	In Stock
100 mg	$496	In Stock	In Stock
500 mg	$1,070	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$89	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.58%

Appearance:Solid

Color:White

Resource Download

COA HPLC HNMR

Product Introduction

evobrutinib AI Summary

evobrutinib exhibits potent inhibitory activity against various tyrosine kinases, notably BTK, TEC, BMX, and BLK, with inhibition percentages ranging from 42% to 90%. It demonstrates strong inhibition of BTK across different assays and cell types: an IC50 of 62.0 nM in full-length human recombinant BTK, 61.0 nM in human THP1 cells, 320.0 nM in human B cells, and 8.9 nM in N-terminal GST-fused human BTK, showing high binding affinity with a Kd of 16.0 nM. The compound also inhibits TEC, BMX, and ERBB4 with IC50 values of 37.9 nM, and shows low inhibition percentages (1%) on EGFR and ERBB2. Selectivity studies reveal higher affinity of evobrutinib for BTK relative to other kinases. Additionally, it demonstrates efficacy in various in vivo and in vitro models, including antiarthritic activity and the inhibition of GP6-mediated platelet aggregation. Despite its potent kinase inhibitory capabilities, evobrutinib shows modest activity against SARS-CoV-2, with low inhibition rates in viral protease and cytotoxicity assays. It exhibits oral bioavailability in animal models, a half-life in plasma, and favorable permeability across human Caco-2 cells. The compound is stable in plasma, maintaining 81.0% stability over 4 hours, and shows relatively high pharmacokinetic stability and favorable selectivity profiles in different experimental setups..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Evobrutinib(M2951) , also known as M-2951 and MSC-2364447C, is a highly selective inhibitor of the Bruton's tyrosine kinase (BTK), which is important in the development and functioning of various immune cells including B -lymphocytes and macrophages. PreClinical research suggests it may be therapeutically useful in certain autoimmune diseases.
Targets&IC50	BTK:37.9 nM
Synonyms	MSC2364447C, M2951

Chemical Properties

Molecular Weight	429.51
Formula	C₂₅H₂₇N₅O₂
Cas No.	1415823-73-2
Smiles	Nc1ncnc(NCC2CCN(CC2)C(=O)C=C)c1-c1ccc(Oc2ccccc2)cc1
Relative Density.	1.227 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 25 mg/mL (58.21 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.66 mM), Sonication is recommended.

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	2.3282 mL	11.6412 mL	23.2823 mL	116.4117 mL
5 mM	0.4656 mL	2.3282 mL	4.6565 mL	23.2823 mL
10 mM	0.2328 mL	1.1641 mL	2.3282 mL	11.6412 mL
20 mM	0.1164 mL	0.5821 mL	1.1641 mL	5.8206 mL
50 mM	0.0466 mL	0.2328 mL	0.4656 mL	2.3282 mL

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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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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