Name | AMD 3465 hexahydrobromide |
Description | AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity. |
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[1].?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[2]. |
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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : 38 mg/mL (42.41 mM) DMSO : 50 mg/mL (55.80 mM), Sonication is recommended.
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Keywords | Inhibitor | AMD 3465 hexahydrobromide | AMD-3465 Hexahydrobromide | GENZ 644494 | AMD3465 | CXCR | HIV | AMD 3465 Hexahydrobromide | GENZ644494 | CXC chemokine receptors | GENZ-644494 hexahydrobromide | inhibit | AMD3465 Hexahydrobromide | AMD-3465 | AMD 3465 | Human immunodeficiency virus | GENZ-644494 |
Inhibitors Related | Stavudine | 5-Fluorouracil | Inosine pranobex | Emtricitabine | Kaempferol | Dolutegravir intermediate-1 | Dextran sulfate sodium salt (MW 4500-5500) | Lamivudine | Chloroquine phosphate | Tenofovir Disoproxil Fumarate | Decanedioic acid | Tenofovir |
Related Compound Libraries | Macrocyclic Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Chemokine Inhibitor Library | Anti-Viral Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |