Home Protein Tyrosine Kinase BTK inhibitor Evobrutinib For research use only.

Evobrutinib

Synonyms: M-2951, MSC-2364447C

Evobrutinib is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.

Evobrutinib Chemical Structure

Evobrutinib Chemical Structure

CAS No. 1415823-73-2

Purity & Quality Control

Batch: S877701 DMSO]86 mg/mL]false]Ethanol]10 mg/mL]false]Water]Insoluble]false Purity: 99.95%
99.95

Evobrutinib Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 Function assay 24 hrs Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by HTRF assay, IC50=0.061μM 32083858
PBMC Function assay 60 mins Inhibition of BTK in human PBMC cells assessed as reduction in anti-IgM-stimulated CD69 expression on B cells preincubated for 60 mins followed by goat F(ab')2 anti-human IgM stimulation and measured after overnight incubation by flow cytometry, IC50=0.061μM 31368705
B cells Function assay 60 mins Inhibition of BTK in human B cells assessed as reduction in anti-IgM/IL4-stimulated CD69 expression on B cells preincubated for 60 mins followed by anti-IgM antibody/IL4 stimulation and measured after 16 hrs by flow cytometry, IC50=0.32μM 32083858
HEK293 Function assay Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by HPLC analysis, Ki=3.1μM 31368705
Sf21 Function assay Inhibition of N-terminal GST-tagged human EGFR (696 to end aminoacids) expressed in baculovirus infected Sf21 cells, IC50=5.8μM 31368705
BTI-TN-5B1-4 Function assay Covalent binding affinity to human BTK (382 to 659 residues) expressed in baculovirus infected BTI-TN-5B1-4 insect cells by isothermal calorimetry 31368705
Sf21 Function assay 1 uM Inhibition of N-terminal His6-tagged full length human BMX expressed in Sf21 cells at 1 uM 31368705
Sf21 Function assay 1 uM Inhibition of N-terminal His6-tagged human TEC (174 to end aminoacids) expressed in baculovirus infected Sf21 cells at 1 uM 31368705
Click to View More Cell Line Experimental Data

Biological Activity

Description Evobrutinib is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.
Targets
BTK [1]
(Cell-free assay)
37.9 nM
In vitro
In vitro

Evobrutinib can inhibit the activity of BTK and prevent the activation of the BCR signaling pathway. It is metabolized via hydroxylation, hydrolysis, O-dealkylation, glucuronidation, and GSH conjugation[2].
In Vivo
In vivo

Evobrutinib is a novel, highly selective, irreversible BTK inhibitor that potently inhibits BCR- and Fc receptor–mediated signaling.
Animal Research Animal Models DBA/1J female mice
Dosages 12 mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05248945 Completed
Healthy
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 January 13 2022 Phase 1
NCT04546789 Completed
Hepatic Impairment
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 September 30 2020 Phase 1
NCT04314024 Completed
Healthy
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 May 25 2020 Phase 1
NCT03934502 Completed
Healthy
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 April 15 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 429.51 Formula

C25H27N5O2
CAS No. 1415823-73-2 SDF --
Smiles C=CC(=O)N1CCC(CC1)CNC2=NC=NC(=C2C3=CC=C(C=C3)OC4=CC=CC=C4)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 86 mg/mL ( (200.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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