Remibrutinib (Synonyms: LOU064)

Name: Remibrutinib
Brand: MedChemExpress
SKU: HY-128757
Rating: 5.0 (5 reviews)

Cat. No.: HY-128757 Purity: 99.76%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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

CAS No. : 1787294-07-8

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

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE Remibrutinib

Cell Proliferation/Viability Assay

Others

In Vivo Efficacy Study

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

: 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

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.

Clinical Trial

Molecular Weight

507.53

Formula

C₂₇H₂₇F₂N₅O₃

CAS No.

1787294-07-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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 (4.10 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.
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 (4.10 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.
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 (4.10 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

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: 99.76%

Select Batch:

Data Sheet (272 KB) SDS (644 KB)

COA (248 KB) HNMR (267 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Remibrutinib 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:

Remibrutinib1787294-07-8LOU064LOU 064LOU-064BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Remibrutinib (Synonyms: LOU064)

Customer Review

Remibrutinib Related Antibodies

5 Publications Citing Use of MCE Remibrutinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Remibrutinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Remibrutinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report