(±)-Zanubrutinib

SKU: orb1679066

Description

(±)-Zanubrutinib is a potent, orally bioavailable small molecule inhibitor of Bruton's tyrosine kinase (Btk). It is widely used in research for investigating B-cell malignancies, demonstrating effective target inhibition in both in vitro and in vivo studies.

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1633350-06-7
• MW: 471.55
• Purity: 98.19% (May vary between batches)
• Formula: C₂₇H₂₉N₅O₃
• SMILES: NC(=O)c1c2NCCC(C3CCN(CC3)C(=O)C=C)n2nc1-c1ccc(Oc2ccccc2)cc1
• Target: BTK
• Solubility: DMSO:50 mg/mL (106.03 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.24 mM);Ethanol:9 mg/mL (19.09 mM)

Bioactivity

• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BTK, BGB3111, BGB-3111, BGB 3111, (±)-BGB-3111, Zanubrutinib

Compound Identifiers

PubChem CID

135905454