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AG-CR1-3620-M005 5 mg INQ
AG-CR1-3620-M025 25 mg INQ
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Additional Information

Product Data
Synonyms PCI-32765
Formula C25H24N6O2
MW 440.5
CAS 936563-96-1
Purity ≥98%
Appearance White solid.
Solubility Soluble in DMSO. Slightly soluble in ethanol (1mg/ml). Insoluble in water.
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

  • Potent and highly selective Bruton's tyrosine kinase (BTK) inhibitor. Orally bioavailable and irreversible inhibitor of BTK (IC50 = 0.5 nM) with antineoplastic activity.
  • Binds to and irreversibly inhibits BTK activity, preventing B cell activation and B cell-mediated signaling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK.
  • Shown to inhibit autophosphorylation of BTK (IC50 = 11nM), phosphorylation of PLCγ (IC50 = 29nM), a substrate of BTK and phosphorylation of ERK (IC50 = 13nM).

Product References

  1. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy: L.A. Honigberg, et al.; PNAS 107, 13075 (2010)
  2. BTK inhibitor ibrutinib is cytotoxic to myeloma and potently enhances bortezomib and lenalidomide activities through NF-κB: S.A. Rushworth, et al.; Cell Signal. 25, 106 (2013)
  3. In vitro, in vivo and ex vivo characterization of ibrutinib: a potent inhibitor of the efflux function of the transporter MRP1: H. Zhang, et al.; Br. J. Pharmacol. 171, 5845 (2014)
  4. Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase: M.S. Davids & J.R. Brown; Future Oncol. 10, 957 (2014) (Review)
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