AMD-3465 is a novel CXCR4 receptor antagonist with potential anticancer and anti-HIV activity. AMD3465 can block infection of T-tropic, CXCR4-using HIV.
Chemical Formula: C24H38N6
Exact Mass: 410.3158
Molecular Weight: 410.59872
Elemental Analysis: C, 70.20; H, 9.33; N, 20.47
Chemical Name: N-(4-((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzyl)-1-(pyridin-2-yl)methanamine hexahydrobromide
InChi Code: InChI=1S/C24H38N6.6BrH/c1-2-13-29-24(5-1)20-28-19-22-6-8-23(9-7-22)21-30-17-4-12-26-15-14-25-10-3-11-27-16-18-30;;;;;;/h1-2,5-9,13,25-28H,3-4,10-12,14-21H2;6*1H
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
AMD-3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells.
AMD-3465 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC50 of 17 nM, but shows no effect on the intracellular calcium fluxes elicited by the CCR5 ligands RANTES, LD78β and MIP-1β in U87.CD4.CCR5 cells.
AMD-3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
AMD-3465 is cytotoxic to the X4 HIV-1 strains IIIB, NL4.3, RF and HE with an IC50 ranging from 6 to 12 nM. The IC50 for suppression of the HIV-2 strains ROD and EHO is 12.3 nM.
AMD-3465 inhibits CXCL-12-induced growth in U87 and Daoy cells. AMD 3465 treatment stimulates the phosphorylation of Erk1/2 in U87 and Daoy cells.
AMD-3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts.
De Silva RA, Peyre K, Pullambhatla M, Fox JJ, Pomper MG, Nimmagadda S. Imaging CXCR4 expression in human cancer xenografts: evaluation of monocyclam 64Cu-AMD3465.JNucl Med. 2011 Jun;52(6):986-93. doi: 10.2967/jnumed.110.085613. PubMed PMID: 21622896; PubMed Central PMCID: PMC3155288.
Bodart V, Anastassov V, Darkes MC, Idzan SR, Labrecque J, Lau G, Mosi RM, Neff KS, Nelson KL, Ruzek MC, Patel K, Santucci Z, Scarborough R, Wong RS, Bridger GJ, Macfarland RT, Fricker SP. Pharmacology of AMD3465: a small molecule antagonist of the chemokine receptor CXCR4. Biochem Pharmacol. 2009 Oct 15;78(8):993-1000. doi: 10.1016/j.bcp.2009.06.010. Epub 2009 Jun 18. PubMed PMID: 19540208.
Hu JS, Freeman CM, Stolberg VR, Chiu BC, Bridger GJ, Fricker SP, Lukacs NW, Chensue SW. AMD3465, a novel CXCR4 receptor antagonist, abrogates schistosomal antigen-elicited (type-2) pulmonary granuloma formation. Am J Pathol. 2006 Aug;169(2):424-32. PubMed PMID: 16877345; PubMed Central PMCID: PMC1599788.
Hatse S, Princen K, De Clercq E, Rosenkilde MM, Schwartz TW,Hernandez-Abad PE, Skerlj RT, Bridger GJ, Schols D. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61. PubMed PMID: 16011832.
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