ONO-4059 free base · Synonyms: Tirabrutinib | GS-4059

Tirabrutinib (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…

For research use only. Not for human or veterinary use.

Target Btk Apoptosis

Research area Inflammation/Immunology Cancer

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Data Sheet SDS COA

ONO-4059 structure

CAS No.: 1351636-18-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 420.00	BP-01873-250mg	In stock	Get quote
500 mg	USD 680.00	BP-01873-500mg	In stock	Get quote
1 g	USD 1,120.00	BP-01873-1g	In stock	Get quote
5 g	Inquire	BP-01873-5g	Inquire	Inquire

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Description

Tirabrutinib (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.

Biological activity

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. 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). Tirabrutinib (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells. 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. Tirabrutinib (6, 20 mg/kg; p.o.; single daily for 3 weeks) shows inhibition of tumour growth in vivo.

Identifiers

SMILES: CC#CC(=O)N1CC[C@H](C1)N1C(=O)N(C2=C(N)N=CN=C12)C1=CC=C(OC2=CC=CC=C2)C=C1
InChIKey: SEJLPXCPMNSRAM-GOSISDBHSA-N

Specifications

MW (average): 454.4806
Formula: C₂₅H₂₂N₆O₃
CAS No.: 1351636-18-4
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

[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.

Same target

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Same research area

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