An irreversible inhibitor of BTK (IC50 = 0.5 nM) that selectively blocks B cell activation

Ibrutinib – 10 mg

Brand:
Cayman
CAS:
936563-96-1
Storage:
-20
UN-No:
Non-Hazardous - /

Bruton’s tyrosine kinase (BTK) is a member of the BTK/Tec family of protein tyrosine kinases involved in signal transduction pathways regulating proliferation, survival, migration, and tissue homing of B-cells.{24859} Ibrutinib is an irreversible inhibitor of BTK (IC50 = 0.5 nM) that selectively blocks B cell activation, promoting apoptosis and preventing homing to the protective tumor microenvironment, at concentrations that do not affect T cell receptor signaling (1,000-fold more potent).{27081,27080} It has been reported to inhibit autophosphorylation of BTK (IC50 = 11 nM), phosphorylation of PLCγ (IC50 = 29 nM), a substrate of BTK, and phosphorylation of ERK (IC50 = 13 nM), a further downstream kinase.{27081} Its use has been examined clinically for the treatment of diseases associated with B cell antigen receptor signaling, including mantle cell lymphoma, chronic lymphocytic leukemia, and non-Hodgkin lymphoma.{24859,27081,24780}  

 

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Description

An irreversible inhibitor of BTK (IC50 = 0.5 nM) that selectively blocks B cell activation, promoting apoptosis and preventing homing to the protective tumor microenvironment, at concentrations that do not affect T cell receptor signaling (1,000-fold more potent); studied clinically for the treatment of diseases associated with B cell antigen receptor signaling, including MCL, CLL, and non-Hodgkin

Formal name: 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one

Synonyms:  Imbruvica|PCI 32765

Molecular weight: 440.5

CAS: 936563-96-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Tec Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Tec Family Signaling||Research Area|Cancer|Tumor Microenvironment||Research Area|Immunology & Inflammation|Adaptive Immunity

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