AMD 3465 (Synonyms: GENZ-644494) |
Catalog No.GC10473
One-Click Copy Product Info
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CXCR4 antagonist,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 185991-24-6
Sample solution is provided at 25 µL, 10mM.
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IC50: 10.38 ± 1.99 nM for CXCR4 activation as measured by GTP binding
CXCR4 is widely expressed in multiple cell types, and involved in neonatal development, hematopoiesis, and lymphocyte trafficking and homing. Additionally CXCR4 is a co-receptor for HIV. Small molecule antagonists of CXCR4 thus have therapeutic potential. AMD3465 is an N-pyridinylmethylene monocyclam CXCR4 antagonist blocking infection of T-tropic, CXCR4-using HIV.
In vitro: Using the CCRF-CEM T-cell line expressing CXCR4 previous authors have demonstrated that AMD3465 is an antagonist of SDF-1 ligand binding, and inhibits SDF-1 mediated signaling as shown by inhibition of GTP binding, calcium flux, and inhibition of chemotaxis. AMD3465 does not inhibit chemokine-stimulated calcium flux in cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7, nor does it inhibit binding of LTB4 to its receptor, BLT1 [1].
In vivo: AMD3465 caused leukocytosis when subcutaneously administered in mice and dogs, with peak mobilization occurring between 0.5 and 1.5 h following subcutaneous dosing in mice and with maximum peak plasma concentration of compound preceding peak mobilization in dogs, demonstrating that AMD3465 has the potential to mobilize hematopoietic stem cells. These data demonstrate the therapeutic potential for the CXCR4 antagonist AMD3465 [1].
Clinical trials: Currenlty no clinical data are available.
Reference:
[1] Bodart V, Anastassov V, Darkes MC, Idzan SR, Labrecque J, Lau G, Mosi RM, Neff KS, Nelson KL, Ruzek MC, Patel K, Santucci Z, Scarborough R, Wong RS, Bridger GJ, Macfarland RT, Fricker SP. Pharmacology of AMD3465: a small molecule antagonist of the chemokine receptor CXCR4. Biochem Pharmacol. 2009;78(8):993-1000.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Hatse S, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005 Sep 1;70(5):752-61. | |
| Cas No. | 185991-24-6 | SDF | |
| Synonyms | GENZ-644494 | ||
| Chemical Name | N-(pyridin-2-ylmethyl)-1-[4-(1,4,8,11-tetrazacyclotetradec-1-ylmethyl)phenyl]methanamine | ||
| Canonical SMILES | C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CNCC3=CC=CC=N3 | ||
| Formula | C24H38N6 | M.Wt | 410.6 |
| Solubility | H2O : ≥ 100 mg/mL (243.55 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4355 mL | 12.1773 mL | 24.3546 mL |
| 5 mM | 487.1 μL | 2.4355 mL | 4.8709 mL |
| 10 mM | 243.5 μL | 1.2177 mL | 2.4355 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)