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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: C25H24N6O2.
Molecular Weight: 440.5.
Purity: >99.5% (HPLC at 214 and 254nm), 100% optical purity (Chiral HPLC), [α]20D = -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.
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