[CAS NO. 155148-31-5]  Plerixaforoctahydrochloride

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PRODUCTS SPECIFICATIONS [155148-31-5]

Catalog
HY-50912
Brand
MCE
CAS
155148-31-5

DESCRIPTION [155148-31-5]

Overview

MDLMFCD04974488
Molecular Weight794.47
Molecular FormulaC28H62Cl8N8
SMILES[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.N1(CCCNCCNCCCNCC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3

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

49 Publications Citing Use of MCE


Summary

Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC 50 of 44 nM.


IC50 & Target

125 I-CXCL12-CXCR4

44 nM (IC 50 )

125 I-CXCL12-CXCR7

HIV-1

1-10 nM (EC 50 )

HIV-2

1-10 nM (EC 50 )


In Vitro

The CXCR4 inhibitor Plerixafor (AMD3100) is a potent inhibitor of CXCL12-mediated chemotaxis (IC 50 , 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] .

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.

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02703779 Siddhartha Ganguly|University of Kansas Medical Center
Multiple Myeloma
March 2016 Phase 2
NCT02056210 University of Padova|Azienda Ospedaliera di Padova
Diabetes
February 2014 Phase 4
NCT00967785 National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC)
Leukopenia|Neutropenia|Infections|Warts|Myelokathexis
January 6, 2010 Phase 1|Phase 2

Appearance

Solid


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:

H 2 O : 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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 120 mg/mL (151.04 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.


Synonyms

1,4,8,11-Tetraazacyclotetradecane, 1,1′-[1,4-phenylenebis(methylene)]bis-, hydrochloride (1:8)
1,4,8,11-Tetraazacyclotetradecane, 1,1′-[1,4-phenylenebis(methylene)]bis-, octahydrochloride
1,1′-[1,4-Phenylenebis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane] hydrochloride (1:8)
JM 3100
SID 791
AMD 3100
Plerixafore 8HCl
AMD 3100 octahydrochloride