1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. Evobrutinib

Evobrutinib  (Synonyms: M2951; MSC2364447C)

Cat. No.: HY-101215 Purity: 98.70%
COA Handling Instructions

Evobrutinib (M2951) est un inhibiteur de BTK qui est oralement actif, puissant, hautement sélectif et irréversiblement covalent, avec un IC50 de 8,9 nM. Evobrutinib (M2951) peut être utilisé pour la recherche sur les maladies auto-immunes.

Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent BTK inhibitor, with an IC50 of 8.9 nM. Evobrutinib (M2951) can be used for the research of autoimmune diseases.

For research use only. We do not sell to patients.

Evobrutinib Chemical Structure

Evobrutinib Chemical Structure

CAS No. : 1415823-73-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 160 In-stock
25 mg USD 290 In-stock
50 mg USD 420 In-stock
100 mg USD 600 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent BTK inhibitor, with an IC50 of 8.9 nM. Evobrutinib (M2951) can be used for the research of autoimmune diseases[1].

IC50 & Target

IC50: 8.9 nM (BTK)[1]

In Vivo

Evobrutinib (0.3, 1, 3, 10, or 30 mg/kg, oral gavage, once daily) demonstrates efficacy in a rat model of rheumatoid arthritis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Lewis rats with semi-established type II collagen arthritis[1].
Dosage: 0.3, 1, 3, 10, or 30 mg/kg.
Administration: Oral gavage once daily for 11 days (days 6-16).
Result: Reduced ankle histopathology scores in a dose-dependent manner, compared to vehicle.
Molecular Weight

429.51

Formula

C25H27N5O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=CC(N1CCC(CNC2=NC=NC(N)=C2C3=CC=C(OC4=CC=CC=C4)C=C3)CC1)=O

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
In Vitro: 

DMSO : 33.33 mg/mL (77.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3282 mL 11.6412 mL 23.2823 mL
5 mM 0.4656 mL 2.3282 mL 4.6565 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.70%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3282 mL 11.6412 mL 23.2823 mL 58.2059 mL
5 mM 0.4656 mL 2.3282 mL 4.6565 mL 11.6412 mL
10 mM 0.2328 mL 1.1641 mL 2.3282 mL 5.8206 mL
15 mM 0.1552 mL 0.7761 mL 1.5522 mL 3.8804 mL
20 mM 0.1164 mL 0.5821 mL 1.1641 mL 2.9103 mL
25 mM 0.0931 mL 0.4656 mL 0.9313 mL 2.3282 mL
30 mM 0.0776 mL 0.3880 mL 0.7761 mL 1.9402 mL
40 mM 0.0582 mL 0.2910 mL 0.5821 mL 1.4551 mL
50 mM 0.0466 mL 0.2328 mL 0.4656 mL 1.1641 mL
60 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9701 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Evobrutinib
Cat. No.:
HY-101215
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