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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $43 | In Stock | In Stock | |
| 10 mg | $71 | In Stock | In Stock | |
| 25 mg | $126 | In Stock | In Stock | |
| 50 mg | $207 | - | In Stock | |
| 100 mg | $369 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $48 | In Stock | In Stock |
| 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, JAK3:5.52 μM, TEC:48 nM, ERBB2:7.31 μM, ERB4:0.77 μM, BLK:0.3 μM, EGFR:3.02 μM, BMX?kinase:6 nM, TXK:92 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] |
| Synonyms | ONO-4059 (hydrochloride), GS-4059 (hydrochloride) |
| Molecular Weight | 490.94 |
| Formula | C25H23ClN6O3 |
| Cas No. | 1439901-97-9 |
| Smiles | Cl.CC#CC(=O)N1CC[C@H](C1)n1c2ncnc(N)c2n(-c2ccc(Oc3ccccc3)cc2)c1=O |
| Relative Density. | no data available |
| Color | White |
| Appearance | Solid |
| 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: 95 mg/mL (193.51 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.07 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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