Mavorixafor trihydrochloride (AMD-070 trihydrochloride)

Alias: Mavorixafor trihydrochloride; AMD-070 trihydrochloride
Cat No.:V51808 Purity: ≥98%
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective, orally available CXCR4 antagonist that can antagonize the binding of 125I-SDF to CXCR4 with an IC50 value of 13 nM.
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) Chemical Structure CAS No.: 2309699-17-8
Product category: CXCR
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Mavorixafor trihydrochloride (AMD-070 trihydrochloride):

  • Mavorixafor (AMD-070)
Official Supplier of:
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Product Description
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective, orally available CXCR4 antagonist that can antagonize the binding of 125I-SDF to CXCR4 with an IC50 value of 13 nM. Mavorixafor trihydrochloride (AMD-070 trihydrochloride) can prevent HIV-1 (NL4.3 strain) replication in MT-4 and PBMCs cells with IC50 values of 1 and 9 nM, respectively.
Biological Activity I Assay Protocols (From Reference)
Targets
125I-SDF-1-CXCR4 ( IC50 = 13 nM ); HIV-1 (NL4.3 strain) ( IC50 = 1 nM ); HIV-1 (NL4.3 strain) ( IC50 = 9 nM ); HIV-1 (NL4.3 strain) ( IC50 = 3 nM ); HIV-1 (NL4.3 strain) ( IC50 = 26 nM )
ln Vitro
Mavorixafor (AMD-070) is an effective and readily available oral CXCR4 antagonist. It inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively, and has an IC50 value of 13 nM against CXCR4 125I-SDF binding. Regarding other chemokine receptors (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2), mavorixafor (AMD-070) exhibits no effect[1]. The growth, migration, and matrigel invasion of B88-SDF-1 cells are significantly suppressed by mavorixafor (AMD-070) at 6.6 µM[2].
ln Vivo
Mavorixafor (AMD-070) (2 mg/kg, p.o.) decreases the expression of human Alu DNA in mice and dramatically reduces the number of metastatic lung nodules in mice without causing a decrease in body weight[2].
Cell Assay
On a 96-well plate, 5 × 103 cells/well are seeded with DMEM containing 10% FCS. The cells are treated with or without 2 µM AMD3100 or 6.6 µM AMD-070 after a 24-hour period. An assay employing MTT is used to quantify the number of cells after 24 or 48 hours[2].
Animal Protocol
Mice: In a pathogen-free environment, BALB/c nude mice are raised. As soon as the mice reach eight weeks of age, the experiments begin. In summary, 1×106 nude mice have their blood vessels inoculated with the cells. Day 49 is the time of the mice's sacrifice. H&E staining is used to determine whether distant metastases are present or absent. The mice are given 0.2 mL of saline as a vehicle or the same volume of Mavorixafor (AMD-070) (2 mg/kg) orally every day as part of their experimental chemotherapy treatment[2].
References

[1]. Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication. J Med Chem. 2010 Apr 22;53(8):3376-88.

[2]. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells. Oncol Rep. 2018 Jul;40(1):303-308.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H30CL3N5
Molecular Weight
458.86
Exact Mass
457.16
CAS #
2309699-17-8
Related CAS #
Mavorixafor; 558447-26-0
Appearance
Powder
SMILES
C1C[C@@H](C2=C(C1)C=CC=N2)N(CCCCN)CC3=NC4=CC=CC=C4N3.Cl.Cl.Cl
InChi Key
FTHQTOSCZZCGHB-VLEZWVESSA-N
InChi Code
InChI=1S/C21H27N5.3ClH/c22-12-3-4-14-26(15-20-24-17-9-1-2-10-18(17)25-20)19-11-5-7-16-8-6-13-23-21(16)19;;;/h1-2,6,8-10,13,19H,3-5,7,11-12,14-15,22H2,(H,24,25);3*1H/t19-;;;/m0.../s1
Chemical Name
N'-(1H-benzimidazol-2-ylmethyl)-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine;trihydrochloride
Synonyms
Mavorixafor trihydrochloride; AMD-070 trihydrochloride
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~150 mg/mL (~326.9 mM)
H2O: ~100 mg/mL (~217.9 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.62 mg/mL (5.71 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.62 mg/mL (5.71 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 0.6 mg/mL (1.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.


Solubility in Formulation 4: ≥ 0.6 mg/mL (1.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 5: ≥ 0.6 mg/mL (1.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 6: 100 mg/mL (217.93 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1793 mL 10.8966 mL 21.7931 mL
5 mM 0.4359 mL 2.1793 mL 4.3586 mL
10 mM 0.2179 mL 1.0897 mL 2.1793 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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