Powder: -20°C for 3 years | In solvent: -80°C for 1 year
(±)-Zanubrutinib ((±)-BGB-3111) is a potent and orally available Bruton's tyrosine kinase (Btk) inhibitor that demonstrates superior oral bioavailability, achieving higher exposure and more complete target inhibi.
説明 | (±)-Zanubrutinib ((±)-BGB-3111) is a potent and orally available Bruton's tyrosine kinase (Btk) inhibitor that demonstrates superior oral bioavailability, achieving higher exposure and more complete target inhibi. |
In vitro | In both biochemical and cellular assays, (±)-Zanubrutinib demonstrates nanomolar Btk inhibition activity. In comparison with ibrutinib, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK. In several MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently 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]. |
別名 | (±)-BGB-3111 |
分子量 | 471.55 |
分子式 | C27H29N5O3 |
CAS No. | 1633350-06-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (106.03 mM)
Ethanol: 9.0 mg/mL (19.1 mM)
You can also refer to dose conversion for different animals. 詳細
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(±)-Zanubrutinib 1633350-06-7 Angiogenesis Tyrosine Kinase/Adaptors BTK BGB-3111 Zanubrutinib BGB 3111 BGB3111 (±)-BGB-3111 Inhibitor inhibitor inhibit