AMD3100 Inhibitor CAS No. 110078-46-1

Cat. No.	Name	Size	Price	Add Cart
KI2220	AMD3100	25 mg	$286
KI2220	AMD3100	100 mg	$858

Chemical Characteristic

Product Name	AMD3100
Synonyms	Plerixafor
CAS No.	110078-46-1
Molecular Weight	502.78
Formula	C₂₈H₅₄N₈
Chemical Name	1,4,8,11-Tetraazacyclotetradecane, 1,1'-[1,4-phenylenebis(methylene)]bis-
Smiles	c1(ccc(cc1)CN1CCNCCCNCCNCCC1)CN1CCNCCCNCCNCCC1
Chemical Structure
Documents	13CNMR HNMR HPLC-220nm HPLC-254nm LSMS

Biological activities

AMD3100 is a selective CXCR4 inhibitor. AMD3100 inhibits 125I-CXCL12 and unlabeled CXCL12 binding to CXCR4 with IC50s of 44 and 1.2 nM, respectively. AMD3100 also potently inhibits CXCL12-mediated chemotaxis with an IC50 of 5.7 nM. In the bare filter migration in vitro, AMD3100 inhibits CXCL12-induced NC-37 cell transendothelial migration (TEM) with an IC50 830 nM.^[1] AMD3100 also modulates the conformation of constitutive CXCR7 homodimers with an EC50 of 46 µM and plays a role as an allosteric modulator of CXCL12 binding to CXCR7.^[2] Importantly, AMD-3100 uniquely inhibits the entry of human immunodeficiency virus type 1 (HIV-1) into CD4_{+ T cells via selective blockade of the chemokine CXCR-4 receptor.^[3] In vitro, AMD3100 significantly suppresses the proliferation of human colorectal cancer cell line SW480 in a dose-dependent manner. AMD3100 (100 and 1000 nM) also significantly inhibits the invasion ability of SW480 cells. In addition, AMD3100 treatment markedly reduces the expression of VEGF and MMP-9 but not MMP-2 in SW480 cells.^[4] In a mouse model of acute promyelocytic leukemia (APL) in vivo, administration of AMD3100 induces a 1.6-fold increase in total leukocytes and a 9-fold increase of circulating APL blast counts. Moreover, treatment of leukemic mice with chemotherapy plus AMD3100 decreases tumor burden and improves overall survival compared with mice treated with chemotherapy alone.^[5]}

Protocols

In vitro: AMD3100 is dissolved in distilled water.^[6]

References

[1] Zabel BA, et al. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol. 2009, 183(5): 3204-3211. [2] Kalatskaya I, et al. AMD3100 is a CXCR7 ligand with allosteric agonist properties. Mol Pharmacol. 2009, 75(5): 1240-1247. [3] Hendrix CW, et al. Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR-4 chemokine receptor, in human volunteers. Antimicrob Agents Chemother. 2000, 44(6): 1667-1673. [4] Li JK, et al. Inhibition of CXCR4 activity with AMD3100 decreases invasion of human colorectal cancer cells in vitro. World J Gastroenterol. 2008, 14(15): 2308-2313. [5] Nervi B, et al. Chemosensitization of acute myeloid leukemia (AML) following mobilization by the CXCR4 antagonist AMD3100. Blood. 2009, 113(24): 6206-6214. [6] Baba M, et al. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc Natl Acad Sci U S A. 1999, 96(10): 5698-5703.

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