Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 1-[(3R)-3-[4-amino-3-[4-(phenoxy-2,3,4,5,6-d5)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C25H19D5N6O2
Formula Weight: 445.5
CAS Number: 1553977-17-5
Notes: Ibrutinib-d5 is intended for use as an internal standard for the quantification of ibrutinib (Item No. 16274) by GC- or LC-MS. Ibrutinib is an irreversible inhibitor of Bruton’s tyrosine kinase (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} Formulations containing it have 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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