Tirabrutinib HCl

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
250mg	$750	Check With Us
500mg	$1350	Check With Us
1g	$2025	Check With Us

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Cat #: V16484 CAS #: 1439901-97-9 Purity ≥ 98%

Description: Tirabrutinib HCl (formerly known as ONO-4059; GS4059; ONO-WG-307; Steboronine), the hydrochloride salt of tirabrutinib, is a selective, covalent/irreversible and orally bioavailable BTK inhibitor approved in Japan for cancer treatment. It inhibits BTK with an IC50 of 2.2 nM. Tirabrutinib covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

References: [1]. Yu H, et al. Bruton's tyrosine kinase inhibitors in primary central nervous system lymphoma-evaluation of anti-tumor efficacy and brain distribution. Transl Cancer Res. 2021 May;10(5):1975-1983.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	490.948
Molecular Formula	C25H23ClN6O3
CAS No.	1439901-97-9
SMILES Code	O=C(N1C[C@@H](CC1)N(C2=O)C3=NC=NC(N)=C3N2C4=CC=C(C=C4)OC5=CC=CC=C5)C#CC.[H]Cl
Synonyms	GS4059; ONO-WG-307; ONO-4059 HCl; GS 4059; ONO4059; ONO 4059; ONO-4059; GS-4059; Tirabrutinib

Protocol	In Vitro	Tirabrutinib hydrochloride (0.1-1000 nM or 0.001-100 nM; 72 h) inhibits the proliferation of OCI-L Y10 and SU-DHL-6 cells with IC50s of 9.127 nM, and 17.10 nM, respectively. Tirabrutinib hydrochloride (0.5, 5, 50 μM; 24, 48 h) induces SU-DHL-6 cells apoptosis needs high dosage and prolonged administration (concentration up to 50 μM and incubates for 48 h). Tirabrutinib hydrochloride (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells.
	In Vivo	Tirabrutinib hydrochloride (10 mg/kg; p.o.; single) is rapidly absorbed into plasma and brain, and reaches Cmax (blood Cmax =339.53 ng/mL; brain Cmax =28.9 ng/mL) 2 hours post administration. Tirabrutinib hydrochloride (6, 20 mg/kg; p.o.; single daily for 3 weeks) shows inhibition of tumour growth in vivo.
	Animal model	Male SD rats (219.0–260.5g)
	Dosages	10 mg/kg
	Administration	Oral administration; single.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.0369 mL	10.1844 mL	20.3688 mL	40.7375 mL
5mM	0.4074 mL	2.0369 mL	4.0738 mL	8.1475 mL
10mM	0.2037 mL	1.0184 mL	2.0369 mL	4.0738 mL
20mM	0.1018 mL	0.5092 mL	1.0184 mL	2.0369 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.