Plerixafor octahydrochloride (Synonyms: AMD3100 octahydrochloride; JM3100 octahydrochloride; SID791 octahydrochloride)

Name: Plerixafor octahydrochloride
Brand: MedChemExpress
SKU: HY-50912
Rating: 5.0 (79 reviews)

Cat. No.: HY-50912 Purity: 99.09%: FAQs
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Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM.

For research use only. We do not sell to patients.

Plerixafor octahydrochloride Chemical Structure

CAS No. : 155148-31-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 92	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 54	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 219	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 417	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 79 publication(s) in Google Scholar

Other Forms of Plerixafor octahydrochloride:

Plerixafor In-stock

67 Publications Citing Use of MCE Plerixafor octahydrochloride

RT-PCR

Proliferation Assay

IHC

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944. [Abstract]; Immunohistochemical staining of proliferation-related protein, Ki-67, in breast cancer after treatment with control, AMD3100 (2.5 mg/kg), Olaparib, or a combination of AMD3100 and Olaparib.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944. [Abstract]; Viability of cells treated with combinations different concentrations of AMD3100 and Olaparib for 24 h.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 4;13(2):118. [Abstract]; PGK1 induced the CXCR4-mediated phosphorylation of AKT (p-AKT) and ERK (p-ERK), and blockade of CXCR4 signaling by AMD3100 (48 h) treatment did not alter cellular PGK1 expression in KIRC cells.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jan 7;6(7):2039-2057. [Abstract]; Western blot analysis of the expression of CXCR4, integrin αvβ3, p-Jak2, Jak2, p-FAK, FAK, p-STAT3 and STAT3 in MSCs (pretreated with a CXCR4 inhibitor (AMD3100; 20 μM; pretreated with 1 h) and an integrin αvβ3 inhibitor (cyclo(-RGDfK))) after the addition of 152RM for 24 h.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633. [Abstract]; Caco-2 cells are incubated with vehicle or AMD3100 (1 µg/ml, 24 hours) after lentivirus transfection (LV-HOXB5), then Western blotting assays are conducted to measure the protein levels of CXCL12, HOXB5, CXCR4, p-ERK and p-ETS1 in the indicated cell lines.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633. [Abstract]; Transwell assays indicated that AMD3100 treatment (1 µg/ml, 24 hours) significantly decreases the migration and invasion of Caco-2-HOXB5 cells.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2020, 2000309.; NOD/SCID mice were i.p. injected with AMD3100 (4 mg/kg). After 1 h, the mice are i.v. injected with iFluor 647-labeled Aazo@CMSN. At 12 h after nanoparticle injection, the mouse craniums are excised for the observation of nanoparticle bone marrow niches targeting under CLSM. Pre-treatment with AMD3100 significantly declined the bone marrow niches targeting of the nanoparticles.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2020 Mar;17(3):283-299. [Abstract]; ELISA of IL-1β in supernatants of BV2 cells stimulated with gp120 LAV (0.5 μg/mL) for 24 h in the presence of increasing doses of a CXCR4-specific inhibitor (AMD3100, 0.1-10 μM; prestimulated with 30 min-2 h).

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037. [Abstract]; IF staining of the tumor tissue sections showed decreased Ki67 and a reversal of EMT markers indicated by increased E-cadherin and decreased N-cadherin expression in the AMD3100 (5 mg/kg or 3.5 mg/kg) treated groups.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037. [Abstract]; Additional EMT-related proteins (Snail and Slug) are downregulated by AMD3100 (5 mg/kg or 3.5 mg/kg) in tumor samples from both diet groups, as quantified by immunoblotting.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;46(3):890-906. [Abstract]; The protein expression of LRRC4, SDF-1, CXCR4, ERK, Slit2 and VEGF in the brain tissue of rats is determined by Western blotting.

: Plerixafor octahydrochloride purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 May 5;13(5):604-614. [Abstract]; Epithelial cells with or without AMD3100 pretreatment are cultured in conditioned medium (CM) from LPS-treated NFs or LTA-treated NFs for 3 days, and the secretion of TNF-α in the supernatant of culture is detected by ELISA. Epithelial cells cultured in MSM are used as control. Both LPS-treated NFs and LTA-treated NFs enhanced the section of TNF-α by epithelial cells compared with control. Pretreatment of epithelial cells with AMD3100 significantly attenuates the increase of TNF-α.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM.

IC₅₀ & Target^[1]^[5]

¹²⁵I-CXCL12-CXCR4

44 nM (IC₅₀)

¹²⁵I-CXCL12-CXCR7

HIV-1

1-10 nM (EC₅₀)

HIV-2

1-10 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.26 μM Compound: 2, AMD3100	Antagonist activity at human recombinant CXCR4 expressed in CHO cells assessed as inhibition of SDF1a-induced electrical impedance by dielectric spectroscopic analysis Antagonist activity at human recombinant CXCR4 expressed in CHO cells assessed as inhibition of SDF1a-induced electrical impedance by dielectric spectroscopic analysis	[PMID: 22909088]
CHO-K1	IC₅₀	> 100 μM Compound: 2, AMD3100	Inhibition of human ERG expressed in CHOK1 cells after 5 mins by whole-cell patch clamp assay Inhibition of human ERG expressed in CHOK1 cells after 5 mins by whole-cell patch clamp assay	[PMID: 22909088]
MT4	EC₅₀	0.002 μM Compound: 2, AMD3100	Antiviral activity against HIV1 infected in MT4 cells expressing CXCR4 assessed as inhibition of virus-induced cytopathic effect after 5 days Antiviral activity against HIV1 infected in MT4 cells expressing CXCR4 assessed as inhibition of virus-induced cytopathic effect after 5 days	[PMID: 22909088]
U-87MG ATCC	IC₅₀	695 nM Compound: 1, AMD-3100	Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis	[PMID: 21105715]

In Vitro

The CXCR4 inhibitor Plerixafor (AMD3100) is a potent inhibitor of CXCL12-mediated chemotaxis (IC₅₀, 5.7 nM) with a potency slightly better than its affinity for CXCR4. Treating the cells with CCX771 or CXCL11 has no effect on CXCL12-mediated MOLT-4 or U937 TEM. In contrast, 10 μM Plerixafor inhibits CXCL12-mediated TEM in both cells lines^[1]. Plerixafor (10 μM)-treated cells show a moderate reduction in cell proliferation compared to CXCL12-stimulated cells, which do not reach statistical significance^[2].

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

In Vivo

Plerixafor (2 mg/kg) administration to UUO mice exacerbates renal interstitial T cell infiltration, resulting in increased production of the pro-inflammatory cytokines IL-6 and IFN-γ and decreased expression of the anti-inflammatory cytokine IL-10^[3]. Both perivascular and interstitial fibrosis are significantly reduced by the CXCR4 antagonist, Plerixafor (AMD3100) at 8 weeks^[4]. LD50, mouse, SC: 16.3 mg/kg; LD50, rat, SC: >50 mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg.

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

Clinical Trial

Molecular Weight

794.47

Formula

C₂₈H₅₄N₈.8HCl

CAS No.

155148-31-5

Appearance

Solid

Color

White to yellow

SMILES

[H]Cl.N1(CCCNCCNCCCNCC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3.[8]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (125.87 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 120 mg/mL (151.04 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.09%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (250 KB) HNMR (256 KB) RP-HPLC (268 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Zabel BA, et al. 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. [Content Brief]

[2]. Mercurio L, et al. 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. [Content Brief]

[3]. Yang J, et al. 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. [Content Brief]

[4]. Chu PY, et al. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616. [Content Brief]

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

Cell Assay ^[2]	U87MG cells are seeded in 96-well plates at the density of 6×10³ cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R, as described in the previous “Treatments” section. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]^[4]	Mice^[3] Male C57bl/6 mice (6-7 weeks old, weighing 20 g) are used. The animals are acclimated to the housing environment, which is SPF and had a temperature of 22°C and a 12h/12h light/dark cycle for a week. Then, they are randomly divided into following experimental groups, with 8 mice in each group: normal (no specific intervention), UUO+AMD3100 (mice received UUO surgery and 2 mg/kg AMD3100), and UUO+PBS (mice received UUO surgery and the same volume of PBS). AMD3100 and PBS are administered via intraperitoneal injection every day until sacrifice. Rats^[4] The CXCR4 antagonist, AMD3100 dissolved in H₂O, is delivered in the type 2 diabetic sand rat model at a dose of 6 mg/kg per day for 8 weeks. In complementary studies, the effect of CXCR4 antagonism (AMD3100 6mg/kg/d) on regulatory T cell numbers is examined. For these studies, AMD3100 or vehicle is delivered via minipump for a period of one week. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zabel BA, et al. 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. [Content Brief] [2]. Mercurio L, et al. 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. [Content Brief] [3]. Yang J, et al. 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. [Content Brief] [4]. Chu PY, et al. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616. [Content Brief] [5]. Schols D, et al. HIV co-receptor inhibitors as novel class of anti-HIV drugs. Antiviral Res. 2006 Sep;71(2-3):216-26. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	1.2587 mL	6.2935 mL	12.5870 mL	31.4675 mL
	5 mM	0.2517 mL	1.2587 mL	2.5174 mL	6.2935 mL
	10 mM	0.1259 mL	0.6294 mL	1.2587 mL	3.1468 mL
	15 mM	0.0839 mL	0.4196 mL	0.8391 mL	2.0978 mL
	20 mM	0.0629 mL	0.3147 mL	0.6294 mL	1.5734 mL
	25 mM	0.0503 mL	0.2517 mL	0.5035 mL	1.2587 mL
	30 mM	0.0420 mL	0.2098 mL	0.4196 mL	1.0489 mL
	40 mM	0.0315 mL	0.1573 mL	0.3147 mL	0.7867 mL
	50 mM	0.0252 mL	0.1259 mL	0.2517 mL	0.6294 mL
	60 mM	0.0210 mL	0.1049 mL	0.2098 mL	0.5245 mL
	80 mM	0.0157 mL	0.0787 mL	0.1573 mL	0.3933 mL
	100 mM	0.0126 mL	0.0629 mL	0.1259 mL	0.3147 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Plerixafor octahydrochloride Related Classifications

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.

Keywords:

Plerixafor octahydrochloride155148-31-5AMD3100 octahydrochlorideJM3100 octahydrochlorideSID791 octahydrochlorideCXCRHIVVirus ProteaseCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusInhibitorinhibitorinhibit

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Plerixafor octahydrochloride (Synonyms: AMD3100 octahydrochloride; JM3100 octahydrochloride; SID791 octahydrochloride)

Customer Review

Other Forms of Plerixafor octahydrochloride:

Plerixafor octahydrochloride Related Antibodies

67 Publications Citing Use of MCE Plerixafor octahydrochloride

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Biological Activity

Protocol

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References

Customer Review

Plerixafor octahydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Plerixafor octahydrochloride Related Classifications

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