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Synonyms: BGB-3111

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $51 | In Stock | In Stock | |
| 2 mg | $77 | In Stock | In Stock | |
| 5 mg | $133 | In Stock | In Stock | |
| 10 mg | $238 | In Stock | In Stock | |
| 25 mg | $455 | In Stock | In Stock | |
| 50 mg | $679 | In Stock | In Stock | |
| 100 mg | $936 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $138 | In Stock | In Stock |
| Description | Zanubrutinib is an oral, irreversible, highly selective Bruton’s tyrosine kinase (BTK) inhibitor (IC₅₀ = 0.3 nM). This agent is used in research on tumors such as lymphoma and leukemia. |
| Targets & IC50 | MOLM-13 cells:5095 nM, HEK293 cells:204.7 nM, BTK:0.3 nM, Ramos cells:1.8 nM, Jurkat cells:3477 nM, Rec1 cells:0.36 nM, TMD8 cells:3.8 nM, OCI-LY1 cells:0.35 nM, Sf9 cells:0.3 nM |
| In vitro | Methods: Human liver microsomes were incubated with 1 μM zanubrutinib, CYP subtype-specific inhibitors, and NADPH for 30 minutes. CYP enzyme phenotypes were analyzed using chemically-inhibited assays. Results: Ketoconazole (a CYP3A inhibitor) significantly inhibited zanubrutinib metabolism, indicating CYP3A as the primary metabolic enzyme. [1] Methods: Lymphoma cell lines Raji, EHEB, JEKO-1, and CD19 CAR-T cells (derived from 7 lymphoma patients) were treated with a concentration gradient of Zanubrutinib (0, 1, 15 μM) for 24 and 48 hours. Cell proliferation inhibition was assessed using the CCK-8 assay. Results: Zanubrutinib exhibited dose-dependent inhibition of proliferation in both lymphoma cells and CAR-T cells. At the low concentration of 1 μM, CAR-T cell inhibition was minimal. [2] |
| In vivo | Methods: Raji cells expressing luciferase were subcutaneously implanted into BALB/c nude mice. Following tumor formation, patients received oral gavage of Zanubrutinib (2.5 mg/kg) twice daily. Results: Zanubrutinib effectively inhibited tumor growth. [2] Methods: Eighteen male Sprague-Dawley rats were randomly divided into three groups and administered via gavage with 0.5% sodium carboxymethylcellulose solvent (control group), fluconazole (20 mg/kg), or itraconazole (20 mg/kg). Thirty minutes later, all rats received oral administration of Zanubrutinib (30 mg/kg). Results: Co-administration of the CYP3A4 inhibitors fluconazole and itraconazole significantly increased both the exposure (AUC) and peak concentration (Cmax) of Zanubrutinib. [3] |
| Synonyms | BGB-3111 |
| Molecular Weight | 471.55 |
| Formula | C27H29N5O3 |
| Cas No. | 1691249-45-2 |
| Smiles | NC(=O)c1c2NCC[C@@H](C3CCN(CC3)C(=O)C=C)n2nc1-c1ccc(Oc2ccccc2)cc1 |
| Relative Density. | 1.33 g/cm3 (Predicted) |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 257.5 mg/mL (546.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.6 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
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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