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PCI-32765 (Ibrutinib) | BTK inhibitor

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Price:
$169.00
Catalog #:
C7327-5
Quantity:


Product Description

PCI-32765 (Ibrutinib) is a selective and irreversible pyrrolopyrimidine-based inhibitor of BTK with IC50 of 0.5 nM. [1] PCI-32765 binds irreversibly to Cys-481 in BTK and thus is only active with other kinases with such a modifiable cysteine residue. In DOHH2 cells, in which the BCR pathway can be activated by anti-IgG, PCI-32765 inhibits autophosphorylation of BTK (IC50, 11 nM), BTK's physiological substrate, PLCg (IC50, 29 nm), and downstream ERK (IC50, 13 nm). [1]


Additionally, PCI-32765 has been shown in CD40- or BCR-activated chronic lymphocytic leukemia cells to inhibit ERK1/2, PI3K, and NFkB. [2] PCI-32765 is efficacious in collagen-induced arthritis models in a dose dependent manner, reversing inflammation at an ED50 of 2.6 mg/kg/day. [3]. PCI-32765 also inhibits BCR-activated primary B-cell proliferation at an IC50 of 8 nM. [3]


Technical information:

Chemical Formula:   C25H24N6O2
CAS #:   936563-96-1
Molecular Weight:   440.5
Purity:   >99%
Appearance:   White
Chemical Name:   (R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one
Solubility:   Up to 100 mM in DMSO
Synonyms:   Ibrutinib, PCI-32765, PCI 32765, PCI32765, CRA-032765

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. 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. 2010, 107(29), 13075-13080. Pubmed ID: 20615965
2. Herman et al., Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood, 2011, 117, 6287-6296. Pubmed ID: 21422473
3. Chang et al., The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res. Ther. 2011, 13(4), R115. Pubmed ID: 21752263

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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