| 货号 | 16274-50mg |
| 描述 | 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.1 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).2,3 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.2 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.1,2,4 |
| 别名 | Imbruvica;PCI 32765; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Leslie, L.A. and Younes, A. Targeting oncogenic and epigenetic survival pathways in lymphoma. Leuk. Lymphoma. 54(11), 2365-2376 (2013). 2.Honigberg, L.A.,Smith, A.M.,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. USA 107(29), 13075-13080 (2010). 3.Herman, S.E.M.,Gordon, A.L.,Hertlein, E., et al. Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood 117(23), 6287-6296 (2011). 4.Wu, M.,Akinleye, A. and Zhu, X. Novel agents for chronic lymphocytic leukemia. J.Hematol.Oncol. 6, 36 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 440.5 |
| 分子式 | C25H24N6O2 |
| CAS号 | 936563-96-1 |
| 稳定性 | ≥ 2 years |
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