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(±)-Zanubrutinib ((±)-BGB-3111) is a potent, orally available Bruton's tyrosine kinase (Btk) inhibitor, exhibiting superior oral bioavailability, higher exposure, and more complete target inhibition.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $42 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $156 | In Stock | |
25 mg | $285 | In Stock | |
50 mg | $455 | In Stock | |
100 mg | $653 | In Stock | |
500 mg | $1,350 | In Stock | |
1 mL x 10 mM (in DMSO) | $108 | In Stock |
Description | (±)-Zanubrutinib ((±)-BGB-3111) is a potent, orally available Bruton's tyrosine kinase (Btk) inhibitor, exhibiting superior oral bioavailability, higher exposure, and more complete target inhibition. |
In vitro | In both biochemical and cellular assays, (±)-Zanubrutinib exhibits nanomolar Btk inhibition activity. Compared to ibrutinib, (±)-Zanubrutinib shows significantly more restricted off-target activities against a panel of kinases, including ITK. In various MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and effectively inhibits cell proliferation[1]. |
In vivo | (±)-Zanubrutinib exhibits dose-dependent anti-tumor properties in mice with REC-1 MCL xenografts, regardless of whether the xenografts are engrafted subcutaneously or through systemic injection via the tail vein. A preliminary 14-day toxicity study in rats indicates that (±)-Zanubrutinib is exceptionally well-tolerated, with a maximally tolerated dose (MTD) remaining undetermined at dosages up to 250mg/kg/day[1]. |
Alias | (±)-BGB-3111 |
Molecular Weight | 471.55 |
Formula | C27H29N5O3 |
Cas No. | 1633350-06-7 |
Smiles | NC(=O)c1c2NCCC(C3CCN(CC3)C(=O)C=C)n2nc1-c1ccc(Oc2ccccc2)cc1 |
Relative Density. | 1.33 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (106.03 mM) Ethanol: 9.0 mg/mL (19.1 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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