Loading... Please wait...

Categories

Our Newsletter


PCI-32765 (Ibrutinib) | BTK inhibitor

  • PCI-32765 (Ibrutinib).jpg
  • PCI-32765 (Ibrutinib), 400x400px, png
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.

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the PCI-32765 (Ibrutinib) | BTK inhibitor to your wish list.

You Recently Viewed...