AMD 3465


Catalog No. Size PriceQuantity
M8716-2 Solid 2 mg $100
M8716-10 Solid 10 mg $300

Description

AMD 3465 is an HIV entry inhibitor which was being developed by AnorMED in the US in conjunction with the Rega Institute of Leuven. AMD 3465 works by antagonizing the HIV-1 entry co-receptor CXCR4. AMD 3465 may be useful for the clinical treatment of HIV-1-infected patients, especially at the late stage of treatment for AIDS patients developing multi-drug-resistant strains.

Product information

CAS Number: 185991-24-6

Molecular Weight: 410.60

Formula: C24H38N6

Synonym:

AMD-3465

GENZ644494

GENZ-644494

GENZ 644494

AMD-8664

Chemical Name: [(pyridin-2-yl)methyl]({4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]phenyl}methyl)amine

Smiles: C(NCC1=CC=CC=N1)C1C=CC(CN2CCNCCCNCCNCCC2)=CC=1

InChiKey: CWJJHESJXJQCJA-UHFFFAOYSA-N

InChi: InChI=1S/C24H38N6/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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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. AMD3465 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.

In Vivo:

AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts.

References:

  1. Hatse S, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61.
  2. Yang L, et al. Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivo. Cancer Res. 2007 Jan 15;67(2):651-8.

Products are for research use only. Not for human use.

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