AG-CR1-3620-M0055 mgCHF 100.00
AG-CR1-3620-M02525 mgCHF 400.00
|Purity Chemicals||≥98% (HPLC)|
|Solubility||Soluble in DMSO. Slightly soluble in ethanol (1mg/ml). Insoluble in water.|
|Shipping and Handling|
|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.|
|Product Specification Sheet|
- 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).
- 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)
- 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)
- 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)
- Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase: M.S. Davids & J.R. Brown; Future Oncol. 10, 957 (2014) (Review)