Evobrutinib (Synonyms: M2951; MSC2364447C)

Name: Evobrutinib
Brand: MedChemExpress
SKU: HY-101215
Rating: 5.0 (6 reviews)

Cat. No.: HY-101215 Purity: 99.60%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1415823-73-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE Evobrutinib

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 8.9 nM (BTK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
TMD8	IC₅₀	56.2 nM Compound: Evobrutinib	Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]

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.

1415823-73-2

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
10 mM	0.2328 mL	1.1641 mL	2.3282 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.60%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (253 KB) HNMR (316 KB) RP-HPLC (146 KB) LCMS (133 KB)

Handling Instructions (2659 KB)

References

[1]. Caldwell R, et al. Discovery of Evobrutinib: An Oral, Potent and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases. J Med Chem. 2019 Aug 1. [Content Brief]

Complete Stock Solution Preparation Table

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

Evobrutinib Related Classifications

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.

Keywords:

Evobrutinib1415823-73-2M2951 MSC2364447CM 2951M-2951BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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Evobrutinib (Synonyms: M2951; MSC2364447C)

Customer Review

Evobrutinib Related Antibodies

6 Publications Citing Use of MCE Evobrutinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Evobrutinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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SAFETY DATA SHEET (SDS)

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