Ibrutinib-d<sub>5</sub>

Ibrutinib-d5

CAT N°: 22561
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From 202.00 171.70

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 PLC? (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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