Name: AMD3465 hexahydrobromide
Brand: BOC Sciences
Rating: 5 (1 reviews)

AMD3465 hexahydrobromide

Category	Human immunodeficiency Virus (HIV)
CAS	185991-07-5
Description	AMD 3465 is a potent and selective 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. MD3465 was even 10-fold more effective as a CXCR4 antagonist, while showing no interaction whatsoever with CCR5. AMD3465 has the potential to mobilize hematopoietic stem cells.

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Product Information

Synonyms

AMD3465; GENZ-644494 hexahydrobromide

Molecular Weight

896.07

Molecular Formula

C24H38N6·6HBr

Canonical SMILES

C1(CNCC2=CC=C(CN3CCNCCCNCCNCCC3)C=C2)=NC=CC=C1.[6HBr]

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

InChIKey

CWJJHESJXJQCJA-UHFFFAOYSA-N

Boiling Point

571.3±50.0 °C at 760 mmHg

Flash Point

299.3±30.1 °C

Purity

≥95%

Density

1.0±0.1 g/cm3

Solubility

Soluble to 50 mM in water and to 25 mM in DMSO.

Appearance

Crystalline Solid

Storage

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

Animal Admin

Two weeks after tumor cell implantation, cohorts of mice with approximately equivalent tumor bioluminescence are divided into equal control and treatment groups. Animals in AMD 3465 experiments receive s.c. osmotic pumps loaded with 10 mg/mL AMD 3465 in sterile PBS or PBS alone. Mice are imaged at least twice after implantation of cells to identify those with equivalent tumor growth rates.

Complexity

413

Exact Mass

410.315796

Index Of Refraction

1.533

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 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.

Target

2G5 mAb-CXCR4:0.75 nM (IC50, in SupT1 cells)
CXCL12AF647-CXCR4:18 nM (IC50, in SupT1 cells)
X4 HIV-1 (IIIB):12.3 nM (IC50, in MT-4 cells)
X4 HIV-1 (NL4.3):6.1 nM (IC50, in MT-4 cells)
X4 HIV-1 (NL4.3AMD3100):2822 nM (IC50, in MT-4 cells)
X4 HIV-1 (RF):7.4 nM (IC50, in MT-4 cells)
X4 HIV-1 (HE):9.8 nM (IC50, in MT-4 cells)
HIV-2 (ROD):12.3 nM (IC50, in MT-4 cells)
HIV-2 (EHO):12.3 nM (IC50, in MT-4 cells)

Vapor Pressure

0.0±1.6 mmHg at 25°C

Description of First Aid Measures

Eye contact

Remove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.

Skin contact

Rinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.

Inhalation

Immediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.

Ingestion

Wash out mouth with water; Do NOT induce vomiting; call a physician.

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