Home Angiogenesis BTK inhibitor tirabrutinib(ONO-4059) hydrochloride For research use only.

tirabrutinib(ONO-4059) hydrochloride

Synonyms: GS-4059

Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is a highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.

tirabrutinib(ONO-4059) hydrochloride Chemical Structure

tirabrutinib(ONO-4059) hydrochloride Chemical Structure

CAS No. 1439901-97-9

Purity & Quality Control

Batch: S816601 DMSO]98 mg/mL]false]Ethanol]1 mg/mL]false]Water]Insoluble]false Purity: 99.77%
99.77

tirabrutinib(ONO-4059) hydrochloride Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

Biological Activity

Description Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is a highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.
Targets
BTK [1]
2.2 nM
In vitro
In vitro

ONO-4059 covalently binds to BTK, and reversibly blocks BCR signaling and B-cell proliferation and activation[1]. It has greater selectivity for BTK than Lck, Fyn, LynA and ONO/GS-4059 only inhibits anti-IgM-induced B-cell activation in a concentration-dependent manner but not inhibit anti-CD3/CD28-induced activation of T-lymphocytes from human PBMCs. ONO/GS-4059 inhibits cell proliferation in some malignant B-cell lines but also induces classical apoptosis at nanomolar concentration in the activated-B cell (ABC) DLBCL cell line, TMD8[4].
Cell Research Cell lines DLBCL cell lines TMD8 cells
Concentrations 320 nM
Incubation Time 48 h
Method

Cells are treated with420 nM, ONO/GS-4059 (320 nM) or in combination for 48 hours and apoptosis is assessed by FITC Annexin V staining, and measured by flow cytometry
In Vivo
In vivo

ONO-4059 demonstrates therapeutic efficacy in a mouse CIA model by suppressing generation of inflammatory chemokines and cytokines including IL-6, IL-8, and TNFα by monocytes, and accompanied by regression of cartilage erosion, bone damage, and pannus formation[1]. In pre-clinical models, and in the clinic in both CLL and NHL patients, It exerts its anti-tumour activity, with a favourable safety profile along with promising efficacy over a long duration[3].
Animal Research Animal Models Male CB17-SCID mice
Dosages 5 and 10 mg/kg
Administration by oral gavage

Chemical Information & Solubility

Molecular Weight 490.94 Formula

C25H22N6O3.HCl
CAS No. 1439901-97-9 SDF Download tirabrutinib(ONO-4059) hydrochloride SDF
Smiles CC#CC(=O)N1CCC(C1)N2C3=NC=NC(=C3N(C2=O)C4=CC=C(C=C4)OC5=CC=CC=C5)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 98 mg/mL ( (199.61 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy tirabrutinib(ONO-4059) hydrochloride | tirabrutinib(ONO-4059) hydrochloride supplier | purchase tirabrutinib(ONO-4059) hydrochloride | tirabrutinib(ONO-4059) hydrochloride cost | tirabrutinib(ONO-4059) hydrochloride manufacturer | order tirabrutinib(ONO-4059) hydrochloride | tirabrutinib(ONO-4059) hydrochloride distributor