1. GPCR/G Protein
  2. CXCR

AMD 3465 hexahydrobromide (Synonyms: GENZ-644494 hexahydrobromide)

Cat. No.: HY-15971 Purity: 98.79%
Handling Instructions

AMD 3465 (hexahydrobromide) is a potent, selective CXCR4 antagonist, and inhibits SDF-1α-ligand binding with Ki of 41.7 nM.

For research use only. We do not sell to patients.
AMD 3465 hexahydrobromide Chemical Structure

AMD 3465 hexahydrobromide Chemical Structure

CAS No. : 185991-07-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in Water USD 95 In-stock
5 mg USD 72 In-stock
10 mg USD 96 In-stock
50 mg USD 312 In-stock
100 mg USD 576 In-stock
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500 mg   Get quote  

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Other Forms of AMD 3465 hexahydrobromide:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


AMD 3465 (hexahydrobromide) is a potent, selective CXCR4 antagonist, and inhibits SDF-1α-ligand binding with Ki of 41.7 nM.

IC50 & Target

Ki: 41.7 nM

In Vitro

The affinity of AMD3465 is 8-fold higher compared with AMD3100, in competition against the radiolabeled monoclonal antibody raised against CXCR4, 12G5. The affinity of AMD3465 is decreased >5000-fold in (D262N)-CXCR4 and 1913-fold in (A175F)-CXCR4. AMD3465 appears to interact with HisVII:-02 at the extracellular end of TM-VII (at the interface to extracellular loop 3) and HisIII:05. Both of these His residues are facing right into the main binding pocket of CXCR4[1]. AMD3465 inhibits 125I-SDF-1α ligand binding to CCRF-CEM cells. AMD3465 inhibits CXCR4 activation as measured by GTP binding with an IC50 of 10.38±1.99 nM, and inhibits SDF-1α mediated calcium flux with an IC50 of 12.07±2.42 nM[2].

In Vivo

AMD3465 (5 mg/kg, s.c.) significantly elevates total white blood cells in DBA/2, C57Bl/6 and BALB/c mice between 0.5 and 2 h. AMD3465 significantly increases the specific cell populations in all three strains of mice included neutrophils, lymphocytes, and monocytes[2].

Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.4355 mL 12.1773 mL 24.3546 mL
5 mM 0.4871 mL 2.4355 mL 4.8709 mL
10 mM 0.2435 mL 1.2177 mL 2.4355 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay

For the competition binding studies against CXCR4, a concentration range of AMD3465 is incubated for 3 h at 4°C in binding buffer (PBS containing 5 mM MgCl2, 1 mM CaCl2, 0.25% BSA pH 7.4) with 5×105 CCRF-CEM cells and 100 pM 125I-SDF-1α in Millipore DuraporeTM filter plates. Unbound 125I-SDF-1α is removed by washing with cold 50 mM HEPES, 0.5 M NaCl pH 7.4. The competition binding assay against BLT1 is performed on membranes from CHO-S cells expressing recombinant BLT1. The membranes is prepisd by mechanical cell lysis followed by high speed centrifugation, resuspended in 50 mM HEPES, 5 mM MgCl2 buffer and flash frozen. The membrane preparation is incubated with AMD3465 for 1 h at room temperature in an assay mixture containing 50 mM Tris, pH 7.4, 10 mM MgCl2, 10 mM CaCl2, 4 nM LTB4 mixed with 1 nM 3H-LTB4 and 8 μg membrane. The unbound 3H-LTB4 is separated by filtration on Millipore Type GF-C filter plates. The bound radioactivity is counted using a LKB Rackbeta 1209 Liquid Scintillation Counter. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay

On the day prior to the experiment, the U87.CD4.CXCR4 transfectants is seeded in 0.1% gelatin-coated 96-well black wall microplates (Costar, Cambridge, MA) at 2×104 cells per well. On the day of the experiment, the cells is loaded with the fluorescent calcium indicator Fluo-3 acetoxymethyl at 4 μM for 45 min at 37°C. After thorough washing with calcium flux assay buffer (Hanks' balanced salt solution with 20 mM Hepes buffer and 0.2% bovine serum albumin, pH 7.4), the cells is preincubated for 15 min at 37°C with AMD3100 or AMD3465 (1 μg/mL) in the same buffer. Then, the intracellular calcium mobilization in response to 2-50 ng/mL CXCL12 is measured at 37°C by monitoring the fluorescence as a function of time simultaneously in all the wells using a Fluorometric Imaging Plate Reader. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

The maximum tolerated dose (MTD) of AMD3465 is determined in mice. AMD3465 is given as a single subcutaneous injection to five male Swiss Webster mice per dose group (5, 10, 20, 50 and 100 mg/kg). Mice is observed for 48 h following administration; evaluations is made of mortality and morbidity, clinical observations, body weight and gross pathology. The pharmacokinetics of AMD3465 in male Swiss Webster mice is determined for a single 25 mg/kg subcutaneous dose. Blood is collected by cardiocentisis from three mice per time point at 0.25, 0.5, 1, 1.5, 2, 4, 8, 12, and 24 h post-administration. Plasma is obtained following centrifugation (3000 rpm, 10 min) and concentrations of AMD3465 in plasma is determined by LC-MS. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight








Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: ≥ 38 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.79%

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