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AMD3465

Chemical Structure : AMD3465

CAS No.: 185991-07-5

AMD3465 (GENZ-644494, AMD3465 hexahydrobromide)

Catalog No.: PC-49202Not For Human Use, Lab Use Only.

AMD3465 (AMD 3465) is a potent, selective monomacrocyclic CXCR4 antagonist with IC50 of 0.75 nM for inhibition of 12G5 mAb binding to CXCR4, dose-dependently inhibits CXCL12 binding in SupT1 cells with IC50 of 18 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AMD3465 (AMD 3465) is a potent, selective monomacrocyclic CXCR4 antagonist with IC50 of 0.75 nM for inhibition of 12G5 mAb binding to CXCR4, dose-dependently inhibits CXCL12 binding in SupT1 cells with IC50 of 18 nM.
AMD3465 inhibits CXCL12-induced calcium signaling in SupT1 cells with IC50 of 17 nM, AMD3465 is >10-fold more potent than AMD3100 in inhibiting calcium mobilization with IC50 of 4 and 58 nM, respectively.
AMD3465 completely failed to block the intracellular calcium fluxes elicited by the CCR5 ligands RANTES, LD78b and MIP-1b in U87.CD4.CCR5 cells.
AMD3465 dose-dependently inhibits intracellular calcium signaling, chemotaxis, CXCR4 endocytosis and mitogen-activated protein kinase phosphorylation induced by CXCL12.
AMD3465 is highly potent against X4 HIV strains (IC50=1-10 nM).
AMD3465 specifically blocks the interaction of HIV gp120 with CXCR4.

Physicochemical Properties

M.Wt 896.082
Formula C24H44Br6N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzyl)-1-(pyridin-2-yl)methanamine hexahydrobromide

References

1. Hatse S, et al. Biochem Pharmacol. 2005 Sep 1;70(5):752-61.

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