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Tirabrutinib

🥰Excellent
Catalog No. TQ0236Cas No. 1351636-18-4
Alias Velexbru, ONO-4059, GS-4059

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.

Tirabrutinib

Tirabrutinib

🥰Excellent
Purity: 99.75%
Catalog No. TQ0236Alias Velexbru, ONO-4059, GS-4059Cas No. 1351636-18-4
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.
Pack SizePriceAvailabilityQuantity
10 mg$43In Stock
25 mg$73In Stock
50 mg$119In Stock
100 mg$223In Stock
200 mg$332In Stock
1 mL x 10 mM (in DMSO)$29In Stock
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Purity:99.75%
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Product Introduction

Bioactivity
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-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].
AliasVelexbru, ONO-4059, GS-4059
Chemical Properties
Molecular Weight454.48
FormulaC25H22N6O3
Cas No.1351636-18-4
SmilesCC#CC(=O)N1CC[C@H](C1)n1c2ncnc(N)c2n(-c2ccc(Oc3ccccc3)cc2)c1=O
Relative Density.1.412 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 90 mg/mL (198 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2003 mL11.0016 mL22.0032 mL110.0158 mL
5 mM0.4401 mL2.2003 mL4.4006 mL22.0032 mL
10 mM0.2200 mL1.1002 mL2.2003 mL11.0016 mL
20 mM0.1100 mL0.5501 mL1.1002 mL5.5008 mL
50 mM0.0440 mL0.2200 mL0.4401 mL2.2003 mL
100 mM0.0220 mL0.1100 mL0.2200 mL1.1002 mL

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