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Tirabrutinib hydrochloride

🥰Excellent
Catalog No. T12311Cas No. 1439901-97-9
Alias ONO-4059 (hydrochloride), GS-4059 (hydrochloride)

Tirabrutinib hydrochloride is a potent, highly selective, and irreversible oral BTK inhibitor. Tirabrutinib hydrochloride irreversibly covalently binds to Bruton tyrosine kinase (BTK) in B cells and exhibits potent in vitro cytotoxicity against many types of B cell malignancies, as well as in vivo antitumor activity in mouse models [1].

Tirabrutinib hydrochloride

Tirabrutinib hydrochloride

🥰Excellent
Purity: 99.27%
Catalog No. T12311Alias ONO-4059 (hydrochloride), GS-4059 (hydrochloride)Cas No. 1439901-97-9
Tirabrutinib hydrochloride is a potent, highly selective, and irreversible oral BTK inhibitor. Tirabrutinib hydrochloride irreversibly covalently binds to Bruton tyrosine kinase (BTK) in B cells and exhibits potent in vitro cytotoxicity against many types of B cell malignancies, as well as in vivo antitumor activity in mouse models [1].
Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$43In Stock
10 mg$71In Stock
25 mg$126In Stock
50 mg$207In Stock
100 mg$369In Stock
1 mL x 10 mM (in DMSO)$48In Stock
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Purity:99.27%
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Product Introduction

Bioactivity
Description
Tirabrutinib hydrochloride is a potent, highly selective, and irreversible oral BTK inhibitor. Tirabrutinib hydrochloride irreversibly covalently binds to Bruton tyrosine kinase (BTK) in B cells and exhibits potent in vitro cytotoxicity against many types of B cell malignancies, as well as in vivo antitumor activity in mouse models [1].
Targets&IC50
BTK:2.2 nM
In vitro
METHODS: Tirabrutinib hydrochloride (0.1-1000 nM or 0.001-100 nM; 72 h) was used to treat DLBCL cell lines SU-DHL-6 and OCI-LY10 to observe the anti-tumor effect on cells.
RESULTS The IC50 values ​​of Tirabrutinib hydrochloride against SU-DHL-6 and OCI-LY10 cell lines were 9.127 μM, and 17.10 μM.[1]
In vivo
Parental TMD8 mice were treated with tirabrutinib (6, 20 mg/kg; p.o.) to confirm whether tirabrutinib remains active in vivo.
RESULTS 0.012% of tirabrutinib resulted in tumor remission in mice. [2]
AliasONO-4059 (hydrochloride), GS-4059 (hydrochloride)
Chemical Properties
Molecular Weight490.94
FormulaC25H23ClN6O3
Cas No.1439901-97-9
SmilesCl.CC#CC(=O)N1CC[C@H](C1)n1c2ncnc(N)c2n(-c2ccc(Oc3ccccc3)cc2)c1=O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 95 mg/mL (193.51 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0369 mL10.1845 mL20.3691 mL101.8454 mL
5 mM0.4074 mL2.0369 mL4.0738 mL20.3691 mL
10 mM0.2037 mL1.0185 mL2.0369 mL10.1845 mL
20 mM0.1018 mL0.5092 mL1.0185 mL5.0923 mL
50 mM0.0407 mL0.2037 mL0.4074 mL2.0369 mL
100 mM0.0204 mL0.1018 mL0.2037 mL1.0185 mL

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