Mavorixafor (AMD-070) triHCl

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
5mg	$140	3-6 Days
10mg	$220	3-6 Days
25mg	$400	3-6 Days
50mg	$650	3-6 Days
100mg	$1050	3-6 Days
250mg	$1650	3-6 Days

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Cat #: V3259 CAS #: 880549-30-4 Purity ≥ 98%

Description: Mavorixafor triHCl (also known as AMD-1107, AMD070, X4P-001) is a potent, selective and orally bioavailable antagonist of CXCR4 with anti-HIV activity. It inhibits CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs. The CXC chemokine receptor CXCR2 is upregulated in a variety of different tumor cell types and involved in tumor cell proliferation and progression. Inhibition of CXCR2 led to reduced metastasis and decreased tumorigenesis. As a CXCR2 antagonist, SX-682 has the potential to treat cancer. AMD-070 has been evaluated in phase I/II studies in different solid tumors by X4 Pharmaceuticals. This compound also has the potential use for the treatment of HIV-1 infection.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	458.86
Molecular Formula	C21H30Cl3N5
CAS No.	880549-30-4
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: >10 mM
	Water: NA
	Ethanol: NA
SMILES Code	NCCCCN(CC1=NC2=CC=CC=C2N1)[C@H]3CCCC4=C3N=CC=C4.[H]Cl.[H]Cl.[H]Cl
Synonyms	X4P-001 3HCl; AMD 11070 3HCl; AMD-070 3HCl; X4P 0013HCl; AMD-11070 3HCl; AMD 070 3HCl; X4P001 3HCl; AMD11070 3HCl; AMD070 3HCl; mavorixafor 3HCl

Protocol	In Vitro	In vitro activity: AMD-070 is active against X4 strain of HIV-1, HIV-1 IIIb in MT-4 cells, and The IC50 values for AMD-070 are 9-fold higher (0.009 μM vs 0.001 μM) and 8.7-fold higher (0.003 μM vs 0.026 μM) in PBMCs compared to MT-4 cells. AMD-070 has antiviral ability with the IC50 value of 15.5 nM. Kinase Assay: SUP-T1 T cells are first preincubated with the compounds (with 1 as a control) for 30 min on ice, washed with PBS with 2% FCS, and incubated with PE-conjugated anti-CXCR4 mAb for 30 min on ice. After being washed with PBS, the cell samples are fixed with 1% paraformaldehyde in PBS and analyzed on a FACS Calibur flow cytometery. The dose-dependent inhibitory effects of the compounds on mAb binding are determined using the mean fluorescence intensity values. Cell Assay: he activated cells (PHA-stimulated blasts) are washed three times with PBS, and viral infections are done. HIV-infected or mock-infected PHA-stimulated blasts are cultured in the presence of 25 U/mL of IL-2 and varying concentrations of compounds. Supernatant is collected at day 10, and HIV-1 core antigen in the culture supernatant is analyzed by the p24 viral Ag ELISA kit. Inhibition of HIV-1 replication in MT-4 cells is performed as previously described. Anti-HIV-1 activity and cytotoxicity measurements are carried out in parallel. They are based on the viability of MT-4 cells that has been infected with HIV-1 in the presence of various concentrations of the test compounds. The ICsub>50 is defined as the concentration required to inhibit 50% of the virus-infected cells against viral cytopathicity.
	In Vivo	AMD-070 shows promising oral bioavailability in rat and dog. The rate of clearance is species dependent with AMD-070 having lower clearance in dog compared to rat.
	Animal model	Rat

These protocols are for reference only. InvivoChem does not independently validate these methods.

Related Biological Data

Pharmacokinetics of AMD070 in the lung of CD-1 mice. PLoS One. 2016 Mar 21;11(3):e0151765.

AMD070 did not alleviate BLM induced lung inflammation at end point as demonstrated by H & E stained lungs. PLoS One. 2016 Mar 21;11(3):e0151765.

PO administration of AMD070 increased leukocyte mobilization. PLoS One. 2016 Mar 21;11(3):e0151765.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.1793 mL	10.8966 mL	21.7931 mL	43.5863 mL
5mM	0.4359 mL	2.1793 mL	4.3586 mL	8.7173 mL
10mM	0.2179 mL	1.0897 mL	2.1793 mL	4.3586 mL
20mM	0.1090 mL	0.5448 mL	1.0897 mL	2.1793 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(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.