AMD 3465 hexahydrobromide

SKU: orb1299977

Description

AMD 3465 hexahydrobromide, also known as GENZ-644494, is a selective CXCR4 chemokine receptor antagonist. It is utilized in oncology and virology research to investigate mechanisms of cancer metastasis and HIV-1 entry in vitro, with studies exploring its potential in preclinical models.

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 185991-07-5
• MW: 896.07
• Purity: 99.39% (May vary between batches)
• Formula: C₂₄H₄₄Br₆N₆
• SMILES: Br.Br.Br.Br.Br.Br.C(NCc1ccccn1)c1ccc(CN2CCCNCCNCCCNCC2)cc1
• Target: CXCR,HIV Protease
• Solubility: DMSO:50 mg/mL (55.8 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.23 mM);H2O:38 mg/mL (42.41 mM)

Bioactivity

• Target IC50:
  HIV-2 (ROD):12.3 nM (IC50, in MT-4 cells)|HIV-2 (EHO):12.3 nM (IC50, in MT-4 cells)|X4 HIV-1 (IIIB):12.3 nM (IC50, in MT-4 cells)|CXCL12 (AF647)-CXCR4:18 nM (IC50, in SupT1 cells)|X4 HIV-1 (HE):9.8 nM (IC50, in MT-4 cells)|X4 HIV-1 (NL4.3):6.1 nM (IC50, in MT-4 cells)|12G5 mAb-CXCR4:0.75 nM (IC50, in SupT1 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)
• In Vivo:
  Administering 2.5 mg/kg/d of AMD 3465 subcutaneously for five weeks significantly inhibits the growth of U87 glioblastoma multiforme (GBM) and Daoy medulloblastoma xenografts.
• In Vitro:
  AMD 3465 hexahydrobromide 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CXCR, CXCL12AF647-CXCR4, CXC chemokine receptors, CXCR4, AMD 3465, AMD 3465 hexahydrobromide, AMD 3465 Hexahydrobromide, AMD3465, AMD-3465, AMD3465 Hexahydrobromide, AMD-3465 Hexahydrobromide, 12G5 mAb-CXCR4, inhibit, Inhibitor, GENZ 644494, GENZ-644494, GENZ-644494 (hexahydrobromide), GENZ-644494 hexahydrobromide, GENZ644494, Human immunodeficiency virus, HIV, HIV Protease, HIVProtease, HIV-2 (EHO), HIV-2 (ROD), X4 HIV-1 (HE), X4 HIV-1 (IIIB), X4 HIV-1 (NL4.3), X4 HIV-1 (NL4.3AMD3100), X4 HIV-1 (RF)

Compound Identifiers

PubChem CID

9897616