PCI-32765

Name: PCI-32765
SKU: P0932
Availability: InStock

Product ID P0932

Cas No. 936563-96-1

Purity ≥99%

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Description

PCI-32765 is an irreversible inhibitor of Bruton’s tyrosine kinase (BTK), an enzyme that plays a significant role in B-cell receptor signaling and B-cell malignancies and autoimmune diseases such as x-linked agammaglobulinemia, chronic lymphocytic leukemia, and non-Hodgkin’s lymphoma. This compound displays anticancer chemotherapeutic, anti-metastatic, immunomodulatory, and anti-fibrotic activities. PCI-32765’s inhibition of BTK prevents IgE-mediated activation of basophils, inhibits signaling from macrophages and mast cells, and inhibits cell migration and survival in cellular and animal models of chronic lymphocytic leukemia. Additionally, PCI-32765 inhibits IL-2-inducible kinase and suppresses the development of fibrosis in pancreatic adenocarcinoma models.

Product Info

Cas No.	936563-96-1
Purity	≥99%
Formula	C₂₅H₂₄N₆O₂
Formula Wt.	440.50
IUPAC Name	1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
Synonym	Ibrutinib
Melting Point	158.3°C
Solubility	DMSO 88 mg/mL (199.77 mM) Ethanol 45 mg/mL (102.15 mM) Water Insoluble
Appearance	White to off white powder

Shipping and Storage

Store Temp	Ambient
Ship Temp	Ambient

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MSDS	P0932 MSDS PDF
Info Sheet	P0932 Info Sheet PDF

References

Massó-Vallés D, Jauset T, Serrano E, et al. Ibrutinib exerts potent antifibrotic and antitumor activities in mouse models of pancreatic adenocarcinoma. Cancer Res. 2015 Apr 15;75(8):1675-81. PMID: 25878147.

Dubovsky JA, Beckwith KA, Natarajan G, et al. Ibrutinib is an irreversible molecular inhibitor of ITK driving a Th1 selective pressure in T-lymphocytes. Blood. 2013 Jul 25. [Epub ahead of print]. PMID: 23886836.

Ponader S, Chen SS, Buggy JJ, et al. The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo. Blood. 2012 Feb 2;119(5):1182-9. PMID: 22180443.

Chang BY, Huang MM, Francesco M, et al. The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther. 2011 Jul 13;13(4):R115. PMID: 21752263.

MacGlashan D Jr, Honigberg LA, Smith A, et al. Inhibition of IgE-mediated secretion from human basophils with a highly selective Bruton's tyrosine kinase, Btk, inhibitor. Int Immunopharmacol. 2011 Apr;11(4):475-9. PMID: 21238622.

Honigberg LA, Smith AM, Sirisawad M, 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 U S A. 2010 Jul 20;107(29):13075-80. PMID: 20615965.

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PCI-32765

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