货号 | 10011332-1mg |
描述 | The α-chemokine receptor, CXCR4, on CD4+ T-cells is used by CXCR4-selective HIV forms as a gateway for T-cell infection. In mammalian cell signaling, CXCR4 activation promotes the homing of hematopoietic stem cells, chemotaxis and quiescence of lymphocytes, and growth and metastasis of certain cancer cell types. Plerixafor (hydrochloride) is a macrocyclic compound that acts as an irreversible antagonist against the binding of CXCR4 with its ligand, SDF-1 (CXCL12). It suppresses infection by HIV with an IC50 value of 1-10 ng/ml1 with selectivity toward CXCR4-tropic virus.2 Plerixafor mobilizes hematopoietic stem and progenitor cells for transplant3 better than the gold standard, G-CSF alone 4 and synergizes with G-CSF.3 It also increases T-cell trafficking in the blood and spleen5 as well as the central nervous system.6 Plerixafor regulates the growth of primary and metastic breast cancer cells7 and inhibits dissemination of ovarian carcinoma cells.8 |
别名 | AMD 3100;JM 3100;Mobozil™;SID 791; |
供应商 | Cayman |
应用文献 | |
1.De Clercq, E.,Yamamoto, N.,Pauwels, R., et al. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrobial Agents and Chemotherapy 38(4), 668-674 (1994). 2.Fransen, S.,Bridger, G.,Whitcomb, J.M., et al. Supression of dualtropic human immunodeficiency virus type 1 by the CXCR4 antagonist AMD3100 is associated with efficiency of CXCR4 use and baseline virus composition. Antimicrobial Agents and Chemotherapy 52(7), 2608-2615 (2008). 3.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). 4.Hess, D.A.,Bonde, J.,Craft, T.C., et al. Human progenitor cells rapidly mobilized by AMD3100 repopulate NOD/SCID mice with increased frequency in comparison to cells from the same donor mobilized by granulocyte colony stimulating factor. Biology of Blood and Marrow Transplantation 13, 398-411 (2007). 5.Bernardini, G.,Sciumè, G.,Bosisio, D., et al. CCL3 and CXCL12 regulate trafficking of mouse bone marrow NK cell subsets. Blood 111(7), 3626-3634 (2008). 6.McCandless, E.E.,Zhang, B.,Diamond, M.S., et al. CXCR4 antagonism increases T cell trafficking in the central nervous system and improves survival from west nile virus encephalitis. Proceedings of the National Academy of Sciences of the United States of America 105(32), 11270-11275 (2008). 7.Smith, M.C.P.,Luker, K.E.,Garbow, J.R., et al. CXCR4 regulates growth of both primary and metastatic breast cancer. Cancer Research 64, 8604-8612 (2004). 8.Kajiyama, H.,Shibata, K.,Terauchi, M., et al. Involvement of SDF-1α/CXCR4 axis in the enhanced peritoneal metastasis of epithelial ovarian carcinoma. International Journal of Cancer 122, 91-99 (2008). | |
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 | 794.5 |
分子式 | C28H54N8 • 8HCl • [XH2O] |
CAS号 | 155148-31-5 |
稳定性 | ≥ 2 years |
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