| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (2.23 mM), Sonication is recommended.
H2O : 38 mg/mL (42.41 mM), Sonication is recommended.
DMSO : 250 mg/mL (279 mM), Sonication is recommended.
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| Keywords | X4 HIV-1 (RF) | X4 HIV-1 (NL4.3AMD3100) | X4 HIV-1 (NL4.3) | X4 HIV-1 (IIIB) | X4 HIV-1 (HE) | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV-2 (ROD) | HIV-2 (EHO) | HIV Protease | HIV | GENZ-644494 hexahydrobromide | GENZ-644494 | GENZ644494 | GENZ 644494 | CXCR4 | CXCR | CXCL12AF647-CXCR4 | CXC chemokine receptors | AMD-3465 Hexahydrobromide | AMD3465 Hexahydrobromide | AMD-3465 | AMD3465 | AMD 3465 hexahydrobromide | AMD 3465 | 12G5 mAb-CXCR4 |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Dolutegravir intermediate-1 | Dimethyl fumarate | Lamivudine | Chloroquine phosphate | Valproic Acid | (-)-Epigallocatechin Gallate | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Tenofovir |
| Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Autophagy Compound Library | Anti-Viral Compound Library | Inhibitor Library | Immuno-Oncology Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
