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Purity: ≥98%
Mavorixafor (AMD-070; AMD11070, AMD070, X4P-001) is an orally bioavailable CXCR4 antagonist with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, it inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs. The proliferation and progression of tumor cells are facilitated by the upregulation of the CXC chemokine receptor CXCR2 in a range of distinct tumor cell types. Reduced tumorigenesis and metastasis were the results of CXCR2 inhibition. SX-682 has the ability to treat cancer because it is a CXCR2 antagonist. AMD-070 has been assessed in phase I/II trials by X4 Pharmaceuticals in various solid tumor types. There may be a further application for this substance in the management of HIV-1 infection.
| Targets |
125I-SDF-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 )
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| Enzyme Assay |
The compounds are first preincubated in SUP-T1 T cells for 30 minutes on ice, with 1 serving as a control. Following this, the cells are washed with PBS containing 2% FCS and then incubated with PE-conjugated anti-CXCR4 mAb for an additional 30 minutes on ice. The cell samples are first fixed with 1% paraformaldehyde in PBS and then examined using an FACS Calibur flow cytometer after being cleaned in PBS. The average fluorescence intensity values are used to calculate the compounds' dose-dependent inhibitory effects on mAb binding.
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| 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].
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| References |
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| Molecular Formula |
C₂₁H₂₇N₅
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| Molecular Weight |
349.47
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| Exact Mass |
349.23
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| Elemental Analysis |
C, 72.17; H, 7.79; N, 20.04
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| CAS # |
558447-26-0
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| Related CAS # |
Mavorixafor trihydrochloride; 2309699-17-8
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| Appearance |
Solid powder
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| SMILES |
C1C[C@@H](C2=C(C1)C=CC=N2)N(CCCCN)CC3=NC4=CC=CC=C4N3
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| InChi Key |
WVLHHLRVNDMIAR-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C21H27N5/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)/t19-/m0/s1
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| Chemical Name |
N'-(1H-benzimidazol-2-ylmethyl)-N'-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| 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 (e.g. under nitrogen), avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
5%DMSO + 40%PEG300 + 5%Tween 80 + 50%ddH2O: 3.5mg/ml (10.02mM) (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8615 mL | 14.3074 mL | 28.6148 mL | |
| 5 mM | 0.5723 mL | 2.8615 mL | 5.7230 mL | |
| 10 mM | 0.2861 mL | 1.4307 mL | 2.8615 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.
Calculation results
Working concentration： mg/mL；
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.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03995108 | Active Recruiting |
Drug: Mavorixafor Drug: Placebo |
WHIM Syndrome | X4 Pharmaceuticals | October 24, 2019 | Phase 3 |
| NCT04154488 | Recruiting | Drug: Mavorixafor | Neutropenia | X4 Pharmaceuticals | October 16, 2020 | Phase 1 Phase 2 |
| NCT06056297 | Not yet recruiting | Drug: Mavorixafor Drug: Placebo |
Neutropenia | X4 Pharmaceuticals | February 2024 | Phase 3 |
| NCT04274738 | Completed | Drug: Mavorixafor Drug: Ibrutinib |
Waldenstrom's Macroglobulinemia | X4 Pharmaceuticals | April 30, 2020 | Phase 1 |
| NCT03005327 | Completed | Drug: X4P-001 | WHIM Syndrome | X4 Pharmaceuticals | December 2016 | Phase 2 |
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