AMD 3465
Based on 5 publication(s) in Google Scholar
AMD 3465 (GENZ-644494) 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.
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- Pureza: 98.24%
- No. CAS: 185991-24-6
- Fòrmula: C24H38N6
- Peso molecular:410.60
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Almacenamiento:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) AMD 3465
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Actividad biológica
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12G5 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) |
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Cell Line
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Type | Value | Description | References |
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| MT4 | CC50 |
>112 μM
Compound: 3d, AMD-3465
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Cytotoxicity against human MT4 cells after 4 days by MTT method
Cytotoxicity against human MT4 cells after 4 days by MTT method
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[PMID: 20043638] |
| MT4 | EC50 |
0.009 μM
Compound: 3d, AMD-3465
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Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay
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[PMID: 20043638] |
| MT4 | EC50 |
1 nM
Compound: 23; AMD3465
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Antiviral activity against HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 4 to 5 days by MTS assay
Antiviral activity against HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 4 to 5 days by MTS assay
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[PMID: 26974376] |
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 (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 185991-24-6
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Appearance Solid-Liquid Mixture
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Peso molecular 410.60
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Fòrmula C24H38N6
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Color Off-white to light yellow
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SMILES
C1(CNCC2=CC=C(CN3CCNCCCNCCNCCC3)C=C2)=NC=CC=C1
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Synonyms
GENZ-644494
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Immunity
Spatiotemporal dynamics of CXCL10 encode contextual immune information revealed by the genetically encoded fluorescent sensor. [Abstract]2025 Sep 9;58(9):2320-2335.e9. PMID: 40818452 -
Br J Haematol
CXCR4 antagonists disrupt leukaemia-meningeal cell adhesion and attenuate chemoresistance. [Abstract]2023 May;201(3):459-469. PMID: 36535585 -
J Labelled Comp Radiopharm
Development of a novel 99m Tc-labeled small molecular antagonist for CXCR4 positive tumor imaging. [Abstract]2018 May 15;61(5):438-446. PMID: 29370457 -
Biomed Pharmacother
AMD3465 (hexahydrobromide) rescues the MG63 osteoblasts against the apoptosis induced by high glucose. [Abstract]2021 Jun:138:111476. PMID: 33773470
AMD 3465 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2021 Jun:138:111476. [Abstract]
The results of western blotting showed that high glucose inhibited the activation of the cell cycle pathway, the expression level of CDK4, CDK6, Nusap1, and Cyclin D1 are reduced. However, under the action of AMD3465 (10 μM), the expression level of proteins is significantly higher than that of the HG group.
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Solvente y solubilidad
H2O : ≥ 100 mg/mL (243.55 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
Following serum starvation for 24 h, astrocytes, granule cells, U87 cells, and Daoy cells are treated with 1 μg/mL CXCL12, 2.5 ng/mL AMD 3465, 200 μM rolipram, or 10 μM forskolin. Daoy and U87 cell growth in culture is measured by trypan blue exclusion after 24 and 48 h of treatment, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Mice are imaged at least twice after implantation of cells to identify those with equivalent tumor growth rates. 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. The infusion rate is 0.25 μL/h (50 μg/d). For the experiments with rolipram or caffeine, mice in the treatment groups receive oral administration of rolipram (5 μg/g/d) or caffeine (100 μg/g/d). The concentration of drug in the water is determined from daily measurements of water consumption by each animal over the course of 7 days. Concentrations are adjusted based on water consumption to provide the prescribed dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hatse S, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61. [Content Brief]
[2]. Yang L, et al. Blocking CXCR4-mediated cyclic AMP suppression inhibits brain tumor growth in vivo. Cancer Res. 2007 Jan 15;67(2):651-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.4355 mL | 12.1773 mL | 24.3546 mL | 60.8865 mL |
| 5 mM | 0.4871 mL | 2.4355 mL | 4.8709 mL | 12.1773 mL | |
| 10 mM | 0.2435 mL | 1.2177 mL | 2.4355 mL | 6.0887 mL | |
| 15 mM | 0.1624 mL | 0.8118 mL | 1.6236 mL | 4.0591 mL | |
| 20 mM | 0.1218 mL | 0.6089 mL | 1.2177 mL | 3.0443 mL | |
| 25 mM | 0.0974 mL | 0.4871 mL | 0.9742 mL | 2.4355 mL | |
| 30 mM | 0.0812 mL | 0.4059 mL | 0.8118 mL | 2.0296 mL | |
| 40 mM | 0.0609 mL | 0.3044 mL | 0.6089 mL | 1.5222 mL | |
| 50 mM | 0.0487 mL | 0.2435 mL | 0.4871 mL | 1.2177 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4059 mL | 1.0148 mL | |
| 80 mM | 0.0304 mL | 0.1522 mL | 0.3044 mL | 0.7611 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2435 mL | 0.6089 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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