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Tirabrutinib

Catalog No. TQ0236 CAS 1351636-18-4

Synonyms: ONO-4059, GS-4059, Velexbru

Tirabrutinib (GS-4059) (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (Btk) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to Btk and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.

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Tirabrutinib, CAS 1351636-18-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 122.00
50 mg	In stock	$ 198.00
100 mg	In stock	$ 372.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.75%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tirabrutinib (GS-4059) (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (Btk) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to Btk and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.
Targets&IC50	BTK:2.2 nM
In vitro	Tirabrutinib (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[1]. Tirabrutinib (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)[1]. Tirabrutinib (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells[2].
In vivo	Tirabrutinib (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[1]. Tirabrutinib (6, 20 mg/kg; p.o.; single daily for 3 weeks) shows inhibition of tumour growth in vivo[2].

Synonyms	ONO-4059, GS-4059, Velexbru
Molecular Weight	454.48
Formula	C25H22N6O3
CAS No.	1351636-18-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90mg/mL (198mM)

References and Literature

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. 2. Kozaki R, et al. Responses to the Selective Bruton's Tyrosine Kinase (BTK) Inhibitor Tirabrutinib (ONO/GS-4059) in Diffuse Large B-cell Lymphoma Cell Lines. Cancers (Basel). 2018 Apr 23;10(4):127. 3. Liclican A, et al. Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition. Biochim Biophys Acta Gen Subj. 2020 Apr;1864(4):129531. 4. Dhillon S. Tirabrutinib: First Approval. Drugs. 2020 Jun;80(8):835-840.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Tyrosine Kinase Inhibitor Library FDA-Approved Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library

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Related compounds with same targets

SB-633825 Avitinib Olmutinib Syk Inhibitor II dihydrochloride Larotinib AZ7550 Vecabrutinib Rilzabrutinib

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Keywords

Tirabrutinib 1351636-18-4 Angiogenesis Tyrosine Kinase/Adaptors BTK ONO4059 ONO-4059 GS 4059 ONO 4059 GS4059 GS-4059 Velexbru inhibitor inhibit

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