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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $39 | In Stock | |
10 mg | $72 | In Stock | |
25 mg | $122 | In Stock | |
50 mg | $198 | In Stock | |
100 mg | $372 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | In Stock |
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-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]. |
Alias | 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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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