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Plerixafor(AMD3100)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Plerixafor(AMD3100)图片
CAS NO:110078-46-1
规格:98%
分子量:502.78
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议

产品介绍
CXCR4 chemokine receptor antagonist
CAS:110078-46-1
分子式:C28H54N8
分子量:502.78
纯度:98%
存储:Store at -20°C

Background:

Plerixafor (AMD3100) is a small-molecule antagonist of CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively [1].


CXCR4 and SDF-1 are key factors in regulating cancer cell invasion and metastasis, and plerixafor can prevent the binding of SDF-1 to CXCR4 for inhibiting cancer metastasis [2]. Plerixafor interfered with CXCL12/CXCR4 mediated retention of hematopoietic stem cells in the bone marrow, and resulted in their mobilization to the blood [3]. Plerixafor amplified the release of circulating neutrophils from the oriented area in the lung, while simultaneously preventing neutrophil returned to the bone marrow [4]. Three adults with WHIM syndrome were subcutaneously injected 0.01 to 0.02 mg/kg plerixafor twice daily for 6 months, circulating leukocytes were constantly increased, and associated with fewer infections [5].


参考文献:
[1]Zabel BA, Wang Y, Lewén S, Berahovich RD, Penfold ME, Zhang P, Powers J, Summers BC, Miao Z, Zhao B, Jalili A, Janowska-Wieczorek A, Jaen JC, Schall TJ. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol. 2009 Sep 1;183(5):3204-11.
[2].Li J, Oupicky D. Effect of biodegradability on CXCR4 antagonism, transfection efficacy and antimetastatic activity of polymeric Plerixafor.Biomaterials. 2014 Jul;35(21):5572-9.
[3]. Broxmeyer HE. Chemokines in hematopoiesis. Curr Opin Hematol. 2008 Jan;15(1):49-58.
[4]. Devi S, Wang Y, Chew WK, Lima R, A-González N, Mattar CN, Chong SZ, Schlitzer A, Bakocevic N, Chew S, Keeble JL, Goh CC, Li JL, Evrard M, Malleret B, Larbi A, Renia L, Haniffa M, Tan SM, Chan JK, Balabanian K, Nagasawa T, Bachelerie F, Hidalgo A, Ginhoux F, Kubes P, Ng LG. Neutrophil mobilization via plerixafor-mediated CXCR4 inhibition arises from lung demargination and blockade of neutrophil homing to the bone marrow. J Exp Med. 2013 Oct 21;210(11):2321-36.
[5]. McDermott DH, Liu Q, Velez D, Lopez L, Anaya-O'Brien S, Ulrick J, Kwatemaa N, Starling J, Fleisher TA, Priel DA, Merideth MA, Giuntoli RL, Evbuomwan MO, Littel P, Marquesen MM, Hilligoss D, DeCastro R, Grimes GJ, Hwang ST, Pittaluga S, Calvo KR, Stratton P, Cowen EW, Kuhns DB, Malech HL, Murphy PM. A phase 1 clinical trial of long-term, low-dose treatment of WHIM syndrome with the CXCR4 antagonist plerixafor. Blood. 2014 Apr 10;123(15):2308-16.