| Name | Tirabrutinib |
| 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. |
| In vitro | Tirabrutinib (0.1-1000 nM or 0.001-100 nM; 72 h) inhibits the proliferation of OCI-LY10 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 apoptosis in SU-DHL-6 cells, requiring high dosage and prolonged administration (up to 50 μM 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, reaching Cmax (blood Cmax = 339.53 ng/mL; brain Cmax = 28.9 ng/mL) 2 hours post-administration[1]. Additionally, Tirabrutinib (6, 20 mg/kg; p.o.; single daily for 3 weeks) inhibits tumor growth in vivo[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 90 mg/mL (198.03 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.26 mM), Sonication is recommended.
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| Keywords | Tirabrutinib | ONO4059 | ONO 4059 | GS4059 | GS 4059 | BTK |
| Inhibitors Related | Stavudine | Cysteamine hydrochloride | Sodium 4-phenylbutyrate | Metronidazole | Citric Acid Triammonium | Tributyrin | L-Methionine | Sodium citrate | Cystamine dihydrochloride | L-Ascorbic acid sodium salt | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Highly Selective Inhibitor Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
