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 ¦ÌM, 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-¦ÊB. 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-¦Á), fibronectin engagement, and stromal cell contact.

June 21, 2017

prudect name : 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 ¦ÌM, 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-¦ÊB. 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-¦Á), fibronectin engagement, and stromal cell contact.
PCI-32765 (Ibrutinib)

Synonyms: PCI-32765 (Ibrutinib)CAS NO: 936563-96-1Molecular Formula: C₂₅H₂₄N₆O₂Molecular Weight: 440.5Purity: 98% minSolubility: In DMSOStorage: -20°C

web site: www.medchemexpress.com