1. GPCR/G Protein Immunology/Inflammation Anti-infection
  2. CXCR HIV
  3. Mavorixafor

Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also 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.

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Mavorixafor Chemical Structure

Mavorixafor Chemical Structure

CAS No. : 558447-26-0

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  • Biological Activity

  • Protocol

  • Purity & Documentation

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Description

Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also 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.

IC50 & Target[1]

125I-SDF-CXCR4

13 nM (IC50)

HIV-1 (NL4.3 strain)

1 nM (IC50, in MT-4 cells)

HIV-1 (NL4.3 strain)

9 nM (IC50, in PBMCs)

HIV-1 (NL4.3 strain)

3 nM (IC90, in MT-4 cells)

HIV-1 (NL4.3 strain)

26 nM (IC90, in PBMCs)

In Vitro

Mavorixafor (AMD-070) is a potent and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also 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. Mavorixafor (AMD-070) shows no effect on other chemokine receptors (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2)[1]. Mavorixafor (AMD-070) (6.6 μM) significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mavorixafor (AMD-070) (2 mg/kg, p.o.) significantly reduces the number of metastatic lung nodules in mice, and lowers the expression of human Alu DNA in mice, without body weight loss[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

349.47

Formula

C21H27N5

CAS No.
Appearance

Solid

Color

White to gray

SMILES

NCCCCN(CC1=NC2=C(N1)C=CC=C2)[C@@H]3C4=C(CCC3)C=CC=N4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    AMD-070 is prepared in oil plus vehicle (PBS) control[3].

In Vivo Dissolution Calculator
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Purity & Documentation
References
Cell Assay
[2]

Cells are seeded on a 96-well plate at 5 × 103 cells/well in DMEM containing 10% FCS. Twenty-four hours later, the cells are treated with or without 2 µM AMD3100 or 6.6 µM AMD-070. After 24 or 48 h, the number of cells is quantified by an assay using MTT[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
BALB/c nude mice are maintained under pathogen-free conditions. The experiments are initiated when the mice are 8 weeks of age. Briefly, the cells are inoculated into the blood vessels of nude mice (1× 106). These mice are sacrificed at day 49. The presence or absence of distant metastases is confirmed by hematoxylin and eosin (H&E) staining. For experimental chemotherapy, the mice are treated by the daily oral administration of 0.2 mL of saline for a vehicle or the same volume of Mavorixafor (AMD-070) (2 mg/kg)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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