Cat. No.: HY-128757

Remibrutinib

(Synonyms: LOU064)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC₅₀ value of 1 nM. Remibrutinib inhibits BTK activity with an IC₅₀ value of 0.023 μM in blood. Remibrutinib has the potential for Chronic urticaria (CU) treatment.

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Pureté: 99.76%
CAS No.: 1787294-07-8
Formule: C₂₇H₂₇F₂N₅O₃
Masse moléculaire:507.53

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Remibrutinib Chemical Structure

CAS No.: 1787294-07-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Essai clinique
Chemical Information
Publications (6)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC₅₀ value of 1 nM. Remibrutinib inhibits BTK activity with an IC₅₀ value of 0.023 μM in blood^[1]. Remibrutinib has the potential for Chronic urticaria (CU) treatment^[2].

IC₅₀ & Target

IC50: 1 nM (BTK)^[1]

In Vitro

In a biochemical enzyme assay,Remibrutinib (example 6) inhibits Btk enzymatic activity with an IC₅₀ value of 1 nM^[1].
In vitro B cell activation assay, Remibrutinib inhibits Btk enzymatic activity in blood with an IC₅₀ value of 0.023 μM, the whole blood is collected from the abdominal aorta of anaesthetized adult male Lewis rats^[1].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1787294-07-8
Appearance Solid
Masse moléculaire 507.53
Formule C₂₇H₂₇F₂N₅O₃
Color White to off-white
SMILES

O=C(NC1=CC(F)=CC(C2=NC=NC(N)=C2OCCN(C)C(C=C)=O)=C1C)C3=CC=C(C4CC4)C=C3F
Synonyms

LOU064
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

All Cell Proliferation/Viability AssayOthersIn Vivo Efficacy Study

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Journal Impact Factor

Blood Adv

BMX kinase mediates gilteritinib resistance in FLT3-mutated AML through microenvironmental factors. [Abstract]

2022 Sep 13;6(17):5049-5060. PMID: 35797240

Remibrutinib purchased from MedChemExpress. Usage Cited in: Blood Adv. 2022 Sep 13;6(17):5049-5060. [Abstract]

MOLM-13 grown under normoxic (−) or hypoxic (+) conditions for 24 hours, followed by treatment with gilteritinib (+) alone or in combination with remibrutinib (3 and 5 μM, respectively) for 48 hours. Cell viability was assessed by MTT (n = 4-6). Representative data of three independent experiments.
ACS Pharmacol Transl Sci

Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]

2025 Mar 12;8(4):917-931. PMID: 40242575
ACS Pharmacol Transl Sci

Synthesis and Preclinical Evaluation of a Novel Fluorine-18-Labeled Tracer for Positron Emission Tomography Imaging of Bruton's Tyrosine Kinase. [Abstract]

2023 Feb 10;6(3):410-421. PMID: 36926452

Remibrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2023 Feb 10;6(3):410-421. [Abstract]

Concentration response of phosphorylated (pBTK) inhibition by PTBTK3 (n = 3) and remibrutinib (n = 3) in JeKo-1 cells.

Remibrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2023 Feb 10;6(3):410-421. [Abstract]

Uptake of [18F]PTBTK3 by JeKo-1 cells in the presence of dimethyl sulfoxide (DMSO) vehicle (n = 3), non-radioactive PTBTK3 (n = 3), or remibrutinib (n = 3).

Remibrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2023 Feb 10;6(3):410-421. [Abstract]

Representative PET images at 60 min post injection of U87MG xenografts (n = 3), JeKo-1 xenografts (n = 3), and JeKo-1 xenografts pre-dosed with remibrutinib (0.1 mg, injected intravenously) (n = 3).

Remibrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2023 Feb 10;6(3):410-421. [Abstract]

ROI analysis of tumor uptake in JeKo-1 xenografts (n = 3), U87MG xenografts (n = 3), and JeKo-1 xenografts pre-dosed with remibrutinib (0.1 mg, injected intravenously) (n = 3) at 60 min post injection.
Biomed Chromatogr

Metabolite profiling of remibrutinib in rat and human liver microsomes using liquid chromatography combined with benchtop orbitrap high-resolution mass spectrometry. [Abstract]

2023 Dec;37(12):e5737. PMID: 37651996
Res Sq

2026 Apr 22.
bioRxiv

2024 September 08.

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (246.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9703 mL

9.8516 mL

19.7033 mL

5 mM

0.3941 mL

1.9703 mL

3.9407 mL

10 mM

0.1970 mL

0.9852 mL

1.9703 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (4.10 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (4.10 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.10 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Daniela Angst, et al. Novel amino pyrimidine derivatives. Patent WO2015079417A1.

[2]. Kolkhir P, et al. New treatments for chronic urticaria. Ann Allergy Asthma Immunol. 2019 Aug 23. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9703 mL	9.8516 mL	19.7033 mL	49.2582 mL
	5 mM	0.3941 mL	1.9703 mL	3.9407 mL	9.8516 mL
	10 mM	0.1970 mL	0.9852 mL	1.9703 mL	4.9258 mL
	15 mM	0.1314 mL	0.6568 mL	1.3136 mL	3.2839 mL
	20 mM	0.0985 mL	0.4926 mL	0.9852 mL	2.4629 mL
	25 mM	0.0788 mL	0.3941 mL	0.7881 mL	1.9703 mL
	30 mM	0.0657 mL	0.3284 mL	0.6568 mL	1.6419 mL
	40 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2315 mL
	50 mM	0.0394 mL	0.1970 mL	0.3941 mL	0.9852 mL
	60 mM	0.0328 mL	0.1642 mL	0.3284 mL	0.8210 mL
	80 mM	0.0246 mL	0.1231 mL	0.2463 mL	0.6157 mL
	100 mM	0.0197 mL	0.0985 mL	0.1970 mL	0.4926 mL

Keywords

Remibrutinib

6 Cited Publications

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Remibrutinib

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Publications Citing Use of MedChemExpress (MCE) Remibrutinib

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Remibrutinib

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Blood Cancer Compound Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Heterocyclic Compound Library

Autoimmune Disease Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Publications Citing Use of MedChemExpress (MCE) Remibrutinib

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Remibrutinib Related Classifications

HY-128757 Related Classifications