Plerixafor 8HCl (AMD3100)

Alias: JM 3100 8HCl;AMD3100; JM 3100; AMD-3100; JM3100; JM-3100; AMD 3100; SDZ-SID-791; JLK-169; SID-791; JM-2987; Plerixafor HCl; MOZOBIL

Cat No.:V1487 Purity: ≥98%

COA Product Data Instructions for use SDS

Plerixafor 8HCl (formerly JM-3100; AMD-3100; SDZ-SID-791; JLK-169; SID-791; JM-2987; MOZOBIL), the hydrochloride salt of Plerixafor, is a specific chemokine receptor CXCR4 antagonist used as an immunostimulant to mobilize hematopoietic stem cells in cancer patients into the bloodstream.

Plerixafor 8HCl (AMD3100) Chemical Structure CAS No.: 155148-31-5
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 Plerixafor 8HCl (AMD3100):

Plerixafor (AMD 3100)

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Biological Activity I Assay Protocols (From Reference)

Targets

¹²⁵I-CXCL12-CXCR4 ( IC50 = 44 nM ); ¹²⁵I-CXCL12-CXCR4; HIV-1 (NL4.3 strain) ( IC50 = 9 nM ); HIV-1 ( EC50 = 1-10 nM ); HIV-2 ( EC50 = 1-10 nM )

ln Vitro

In vitro activity: Plerixafor (AMD3100), an inhibitor of CXCR4, is a strong inhibitor of CXCL12-mediated chemotaxis (IC50, 5.7 nM), with a potency that is marginally higher than its affinity for CXCR4. CXCL12-mediated MOLT-4 or U937 TEM is unaffected by CCX771 or CXCL11 treatment of the cells. On the other hand, 10 μM Plerixafor inhibits both cell lines' CXCL12-mediated TEM[1]. Comparing Plerixafor (10 μM)-treated cells to CXCL12-stimulated cells, which do not reach statistical significance, the former exhibit a moderate reduction in cell proliferation[2].

ln Vivo

Plerixafor (2 mg/kg) administration to UUO mice intensifies the infiltration of renal interstitial T cells, leading to elevated levels of pro-inflammatory cytokines, such as IL-6 and IFN-γ, and lowered expression of anti-inflammatory cytokine, IL-10[3]. At eight weeks, the CXCR4 antagonist Plerixafor (AMD3100) significantly reduces both interstitial and perivascular fibrosis[4]. LD50: 16.3 mg/kg for mice; >50 mg/kg for rats; 5.2 mg/kg for mice and rats administered intravenously.

Cell Assay

U87MG cells are treated with CXCL12, Plerixafor, or peptide R, as mentioned in the previous "Treatments" section, after being seeded in 96-well plates at a density of 6x103 cells in 200 μL/well. During the last two hours of treatment, MTT (5 μg/mL) is added at 24, 48, and 72 hours. Following the removal of the cell medium, 100 μL of DMSO is added, and an LT-4000MS Microplate Reader is used to measure the optical densities at 595 nm. Triplicate measurements are taken from three separate experiments[2].

Animal Protocol

Mice: The mice used are male C57bl/6s, aged 6-7 weeks and weighing 20 g. After a week of a 22°C temperature and a 12 hr /12 hr light/dark cycle, the animals are acclimated to their new home in SPF. Next, they are split into three experimental groups at random, each containing eight mice: normal (no special treatment), UUO+AMD3100 (mice that underwent UUO surgery plus 2 mg/kg AMD3100), and UUO+PBS (mice that underwent UUO surgery plus the same amount of PBS). Every day until sacrifice, intraperitoneal injections of AMD3100 and PBS are given.
Rats: In the type 2 diabetic sand rat model, the CXCR4 antagonist AMD3100 dissolved in H₂O is administered at a dose of 6 mg/kg per day for eight weeks. The impact of CXCR4 antagonism (AMD3100 6mg/kg/d) on the quantity of regulatory T cells is investigated in complementary investigations. For the duration of one week, the AMD3100 or vehicle is supplied via minipump for these investigations.

References

[1]. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol. 2009 Sep 1;183(5):3204-11.

[2]. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55.

[3]. Continuous AMD3100 Treatment Worsens Renal Fibrosis through Regulation of Bone Marrow Derived Pro-Angiogenic Cells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926.

[4]. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616.

[5]. HIV co-receptor inhibitors as novel class of anti-HIV drugs. Antiviral Res. 2006 Sep;71(2-3):216-26.

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

Physicochemical Properties

Molecular Formula

C28H54N8.8HCL

Molecular Weight

794.47

Exact Mass

794.25

Elemental Analysis

C, 42.33; H, 7.87; Cl, 35.70; N, 14.10

CAS #

155148-31-5

Related CAS #

Plerixafor; 110078-46-1

Appearance

White solid powder

SMILES

C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3.Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl

InChi Key

UEUPDYPUTTUXLJ-UHFFFAOYSA-N

InChi Code

InChI=1S/C28H54N8.8ClH/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36;;;;;;;;/h5-8,29-34H,1-4,9-26H2;8*1H

Chemical Name

1-[[4-(1,4,8,11-tetrazacyclotetradec-1-ylmethyl)phenyl]methyl]-1,4,8,11-tetrazacyclotetradecane;octahydrochloride

Synonyms

JM 3100 8HCl;AMD3100; JM 3100; AMD-3100; JM3100; JM-3100; AMD 3100; SDZ-SID-791; JLK-169; SID-791; JM-2987; Plerixafor HCl; MOZOBIL

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

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: <1 mg/mL

Water: ~100 mg/mL (~125.9 mM)

Ethanol: <1 mg/mL

Solubility (In Vivo)

Saline: 30 mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.2587 mL	6.2935 mL	12.5870 mL
	5 mM	0.2517 mL	1.2587 mL	2.5174 mL
	10 mM	0.1259 mL	0.6294 mL	1.2587 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.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

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Concentration (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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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.

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.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06141304	Active Recruiting	Drug: Plerixafor	Relapsed Adult ALL Relapsed Adult AML	The First Hospital of Jilin University	September 1, 2023	Phase 2
NCT02193191	Active Recruiting	Drug: Plerixafor	Sickle Cell Disease	Memorial Sloan Kettering Cancer Center	September 2014	Phase 1
NCT03182426	Active Recruiting	Drug: Plerixafor Drug: Alemtuzumab	Diabetes Mellitus, Type 1	University of Alberta	August 15, 2017	Phase 1 Phase 2
NCT03653247	Active Recruiting	Drug: Busulfan Biological: Plerixafor	Sickle Cell Disease	Sangamo Therapeutics	March 6, 2019	Phase 1 Phase 2
NCT02570542	Active Recruiting	Drug: Plerixafor Drug: G-CSF	Myeloma	University of Chicago	July 12, 2011	Phase 1

Biological Data

Wound-healing in diabetic mice. J Invest Dermatol. 2012 Mar;132(3 Pt 1):711-20.
Mobilization of bone marrow–derived cells. J Invest Dermatol. 2012 Mar;132(3 Pt 1):711-20.
Activity and mRNA expression in 3T3 fibroblasts after treatment with AMD3100. J Invest Dermatol. 2012 Mar;132(3 Pt 1):711-20.