PCI-32765 Racemate

PCI-32765 Racemate

Catalog Number:
L002370466APE
Mfr. No.:
APE-B3242
Price:
$402
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      • Overview
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          Background

          PCI-32765 is an inhibitor of Bruton tyrosine kinase (BTK) with IC50 value of 0.5nM [1].PCI-32765 is a covalent and irreversible inhibitor of BTK through bonding to Cys-481 in the ATP binding domain. PCI-32765 inhibits phosphorylation of BTK in a B cells (IC50 of 11nM) as well as the downstream substrates phosphoinositide phospholipase Cγ (PLC γ) and ERK in cell assays. PCI-32765 has in vivo efficacy in B cell lymphoma. In CLL cells, PCI-32765 induces cells apoptosis through inhibiting the expression of BCR-dependent UDP-glucose ceramide glucosyltransferase [1]. PCI-32765 is oral effective in vivo. It induces lymphocytosis during the first weeks of therapy in patients with CLL. It is also efficacious in autoimmune disease. In the MRL-Fas lupus model, PCI-32765 inhibits collagen-induced arthritis as well as autoantibody production and development of kidney disease. It also diminished FcγRIII-induced production of pro-inflammatory cytokines [1].

          [1] Burger JA, Buggy JJ. Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765). Leuk Lymphoma. 2013 Nov;54(11):2385-91.

      • Properties
        • Alternative Name
          1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
          CAS Number
          936563-87-0
          Molecular Formula
          C25H24N6O2
          Molecular Weight
          440.5
          Purity
          98.00%
          Solubility
          Soluble in DMSO
          Storage
          Store at RT

          * For Research Use Only

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