Ibrutinib

CHF 140.00
In stock
AG-CR1-3620-M0055 mgCHF 140.00
AG-CR1-3620-M02525 mgCHF 390.00
 
More Information
Product Details
Synonyms PCI-32765
Product Type Chemical
Properties
Formula C25H24N6O2
MW 440.5
CAS 936563-96-1
Purity Chemicals ≥98% (HPLC)
Appearance White solid.
Solubility Soluble in DMSO. Slightly soluble in ethanol (1mg/ml). Insoluble in water.
InChi Key XYFPWWZEPKGCCK-GOSISDBHSA-N
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.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • 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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