Ibrutinib, Free Base (CRA-032765, Imbruvica, PCI-32765, CAS 936563-96-1), >99%

LC Laboratories' Product Number I-3311 - Ibrutinib, Free Base (CRA-032765, Imbruvica, PCI-32765, CAS 936563-96-1), >99% - for research use only. Ibrutinib, also known as PCI-32765, is a selective and irreversible inhibitor of the enzyme Bruton's tyrosine kinase (BTK). It inhibited BTK potently, with an IC50 of 0.72 nM in enzymology assays and with an IC50 of 10 nM in cellular assay with Ramos cells. It demonstrated preference toward BTK over closely related kinases, blocked B cell function and BTK-dependent processes, and demonstrated clear efficacy in a mouse arthritis model. Ibrutinib blocked B-cell antigen receptor (BCR) signaling in human peripheral B cells at concentrations which did not change T cell receptor signaling, reduced the level of circulating autoantibodies and completely suppressed collagen-induced arthritis in mice, inhibited the production of autoantibodies and the development of kidney disease in the MRL-Fas(lpr) lupus model, and induced objective clinical responses in dogs with spontaneous B-cell non-Hodgkin lymphoma. Active site occupancy of BTK was closely correlated with the inhibition of BCR signaling and in vivo efficacy. Ibrutinib was well tolerated and had significant activity in patients with relapsed/refractory B-cell malignancies. Ibrutinib is the active ingredient in the drug product sold under the trade name Imbruvica®. This drug is currently approved in at least one country for use in patients with mantle cell lymphoma and chronic lymphocytic leukemia. NOTE: THE IBRUTINIB, FREE BASE RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT IMBRUVICA®, AND IS NOT FOR HUMAN USE.

• Supplier: LC Laboratories
• Product #: I-3311
• Sku #: I-3311_5g