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Product Details

Ibrutinib | BTK inhibitor

Ibrutinib (936563-96-1) is a very potent (IC50 = 0.5nM) irreversible inhibitor of Bruton tyrosine kinase (BTK) that blocks activation of the B-cell antigen receptor (BCR).1 Ibrutinib also potently inhibits several other kinases including BLK, BMS, FGR, EGFR, and ITK.  It is a clinically useful drug to treat B cell cancers. It inhibits CLL cell migration and survival2,3 and downregulates expression of CD204.  It enhanced antitumor immune responses in combination with anti PD-L1 blockade via its inhibition of ITK (IL2-inducible T-cell kinase).5

References/Citations

1) Honigberg et al. (2010), 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. USA 107 13075
2) Ponader et al. (2012), The Bruton tyrosine kinase Inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo; Blood 119 1182
3) De Rooij et al. (2012), The clinically active BTK inhibitor PCI-32765 targets B-cell receptor- and chemokine-controlled adhesion and migration in chronic lymphocytic leukemia; Blood 119 2590
4) Pavlasoca et al. (2016), Ibrutinib inhibits CD20 upregulation on CLL B cells mediated by the CXCR4/SDF-1 axis; Blood 128 1609
5) Sagiv-Barfi et al. (2015), Therapeutic antitumor immunity by checkpoint blockade is enhanced by ibrutinib, an inhibitor of both BTK and ITK; Proc. Natl. Acad. Sci. USA 112 E966
6) Weber et al. (2017), Bruton's Tyrosine Kinase: An Emerging Key Player in Innate Immunity, Front. Immunol. 1454

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Catalog#  10-4757-0010

$40.00
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CAS:
936563-96-1
Catalog Number:
10-4757
Alternate Name:
PCI-32765
Activity:
BTK inhibitor/Cancer immunotherapy enhancer
Chemical Name:
1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
Molecular Weight:
440.51
Molecular Formula:
C25H24N6O2
Solubility:
Soluble in DMSO ( up to at least 25 mg/ml)
Physical Properties:
White or off-white solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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