货号 | 17993-50mg |
描述 | Bruton’s tyrosine kinase (BTK) is a non-receptor tyrosine kinase involved in signal transduction pathways regulating the proliferation, activation, and differentiation of B cells. AVL-292 is an orally available, selective, and irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481, thereby preventing its activity.1,2 AVL-292 has been shown to inhibit osteoclast function and to reduce osteoclast-stimulated proliferation of multiple myeloma cells in animal models of rheumatoid arthritis and multiple sclerosis, both of which are diseases where B cells play an important role.2,3 In clinical trials, AVL-292 has demonstrated therapeutic significance in the treatment of both B cell-related cancers (e.g., non-Hodgkin’s lymphoma and B cell chronic lymphocytic leukemia) and autoimmune diseases (e.g., rheumatoid arthritis).2,4,3 |
别名 | CC-292;Spebrutinib; |
供应商 | Cayman |
应用文献 | |
1.Evans, E.K.,Tester, R.,Aslanian, S., et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. Journal of Pharmacology and Experimental Therapeutics 346(2), 219-228 (2013). 2.Aalipour, A. and Advani, R.H. Bruton tyrosine kinase inhibitors: A promising novel targeted treatment for B cell lymphomas. British Journal of Haematology 163(4), 436-443 (2013). 3.DCruz, J.J. and Uckun, F.M. Novel Bruton’s tyrosine kinase inhibitors currently in development. OncoTargets and Therapy 6, 161-176 (2013). 4.Burger, A. Bruton’s tyrosine kinase (BTK) inhibitors in clinical trials. Curr.Hematol.Maliq.Rep. 9(1), 44-49 (2014). | |
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 | 423.4 |
分子式 | C22H22FN5O3 |
CAS号 | 1202757-89-8 |
稳定性 | ≥ 2 years |
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