PCI-32765 (IBRUTINIB)

Background Information:

B-cell antigen receptor (BCR) signaling is required for tumor
expansion and proliferation. Bruton’s Tyrosine Kinase (BTK) is an
essential element of the BCR signaling pathway. Containment of BTK
blocks BCR signaling and induces apoptosis. PCI-32765 is a potent,
selective and orally bioavailable irreversible inhibitor of BTK with IC₅₀ value of 0.5 nM.

Reference:

1. H. Zhang, et al, In vitro, in vivo and ex vivo characterization of
ibrutinib: a potent inhibitor of the efflux function of the transporter
MRP1, Br J Pharmacol. 2014 Dec;171(24):5845-57.
2. LA Honigberg, et al, The Bruton tyrosine kinase inhibitor PCI-32765
blocks B-cell activation and is efficacious in models of autoimmune
disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul
20;107(29):13075-80.* Our product PCI-32765 (Ibrutinib) has been through
a thorough analysis and characterization – HPLC-MS, Chiral HPLC, NMR,
optical rotation measurement (Degree and Direction) and Quantitative
Elemental Analysis, a superior product in every aspect.

APIM050220: PCI-32765 (IBRUTINIB)

CAS No.: 936563-96-1.
Molecular Formula: C₂₅H₂₄N₆O_2.
Molecular Weight: 440.5.
Purity: >99.5% (HPLC at 214 and 254nm), 100% optical purity (Chiral HPLC), [α]²⁰_D = -128 ^o (c 0.87, Chloroform).
QC: HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.