| 货号 | 11959-25mg |
| 描述 | C-X-C chemokine receptor type 4 is a receptor for the stromal cell-derived factor-1 which is designated as chemokine ligand 12 (CXCL12). It is involved in cell progression, hematopoiesis, cancer, HIV entry, and rheumatoid arthritis.1,2,3 AMD 3465 blocks the cell surface binding of CXCL12 with an IC50 value of 18 nM.4 It inhibits CXCL12-induced calcium mobilization (IC50 = 4 nM) and at 6,250 nM completely blocks CXCL12-induced chemotaxis of SupT1 cells.4 AMD 3465 is active against various HIV strains with IC50 values ranging from 6 to 12 nM.4 It dose dependently inhibits eosinophil recruitment during type-2 granuloma formation and interferes with primary and secondary T-cell activation events in lymphoid tissue.5 At 50 μg/day, AMD 3465 blocks tumor growth and prevents CXCL12-induced cAMP suppression in xenograft models of medulloblastoma and glioblastoma.6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Broxmeyer, H.E.,Orschell, C.M.,Clapp, D.W., et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. Journal of Experimental Medicine 201(8), 1307-1318 (2005). 2.Dorsam, R.T., and Gutkind, J.S. G-protein-coupled receptors and cancer. Nature Reviews.Cancer 7, 79-94 (2007). 3.Tamamura, H.,Hiramatsu, K.,Ueda, S., et al. Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131. Journal of Medicinal Chemistry 48, 380-391 (2005). 4.Hatse, S.,Princen, K.,De Clercq, E., et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochemical Pharmacology 70, 752-761 (2005). 5.Hu, J.S.,Freeman, C.M.,Stolberg, V.R., et al. AMD3465, a novel CXCR4 receptor antagonist, abrogates schistosomal antigen-elicited (type-2) pulmonary granuloma formation. American Journal of Pathology 169(2), 424-432 (2006). 6.Yang, L.,Jackson, E.,Woerner, B.M., et al. Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivo. Cancer Research 67(2), 651-658 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 896.1 |
| 分子式 | C24H38N6 • 6HBr |
| CAS号 | 185991-07-5 |
| 稳定性 | ≥ 2 years |
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