Home Products PCI-32765 (Ibrutinib)
PCI-32765 (Ibrutinib)
Synonyms: PCI-32765 (Ibrutinib)
CAS NO: 936563-96-1
Molecular Formula: C25H24N6O2
Molecular Weight: 440.5
Purity: 98% min
Solubility: In DMSO
Storage: -20°C
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Remarks: PCI-32765 is a high potent irreversible BTK inhibitor with an IC50 of 0.46 nM for the purified Btk.PCI-32765 is highly active and well tolerated in CLL/SLL pts irrespective of high risk genomic abnormalities. Although follow-up is short, the high response rate and very low progression rate suggests that PCI-32765 may be an important new targeted treatment approach for CLL pts. In ex vivo assays with whole bold, PCI-32765 prevents the activation of human BCR with an IC50 of about 0.2 M, while not influencing the activation of T cell. Treatment of CD40 or BCR activated CLL cells with PCI-32765 results in inhibition of BTK tyrosine phosphorylation and also effectively abrogates downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-B. In addition, PCI-32765 prevents activation-induced proliferation of CLL cells in vitro, and effectively inhibits survival signals provided externally to CLL cells from the microenvironment including soluble factors (CD40L, BAFF, IL-6, IL-4, and TNF-), fibronectin engagement, and stromal cell contact.

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