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110078-46-1 (Plerixafor)

1

Identification

Plerixafor Plerixafor
Name Plerixafor
Formula C28H54N8
MW 502.78
CAS No. 110078-46-1
EINECS
Smiles C1(CN2CCCNCCNCCCNCC2)=CC=C(C=C1)CN3CCNCCCNCCNCCC3
Synonyms AMD3100; Mozobil; JM-3100;AMD-3100;AMD 3100;JM 3100;JM3100; 1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)benzene
InChI InChI=1S/C28H54N8/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
2

Introduction

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively. IC50 value: 44 nM (CXCR4); 5.7 nM (CXCL12-mediated chemotaxis) Target: CXCR4 in vitro: Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4.

Background Information

Chemokine receptor CXCR4 antagonist ......by AOBIOUS INC
Plerixafor 8HCl (AMD3100 8HCl) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively. In vitro, Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. ......by AbMole BioScience
Plerixafor is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4. The CXCR4 alpha-chemokine receptor and one of its ligands, SDF-1, are important in hematopoietic stem cell homing to the bone marrow and in hematopoietic stem cell quiescence. CXCR-4 antagonist Plerixafor is one of the most efficient bone marrow stem cell mobilizers. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor results in the rapid and reversible mobilization of hematopoietic stem cells into the peripheral circulation and is synergistic when combined with G-CSF. ......by AbMole BioScience
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation. ......by AdooQ BioScience, LLC
Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively. ......by BOC Sciences
Plerixafor is a selective CXCR4 antagonist with IC50 of 44 nM. ......by MedChemexpress Co., Ltd.
Plerixafor (INN and USAN, trade name Mozobil) is an immunostimulant used to mobilize hematopoietic stem cells in cancer patients into the bloodstream. The stem cells are then extracted from the blood and transplanted back to the patient. ......by MedKoo Biosciences, Inc.
Plerixafor (JM-3100, AMD-3100, SID-791) is a potent, selective CXCR4 inhibitor (IC50=44 nM) that inhibits the replication of various HIV-1 and HIV-2 strains in various cell lines with EC50 of 10ng/ml; can produce mesenchymal stem cells and endothelial progenitor cells in mice in combination with VEGF; also is an allosteric agonist of CXCR7.Blood CancerApproved ......by ProbeChem
Plerixafor (AMD3100) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. ......by Selleck Chemicals LLC
Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity. Plerixafor blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models Twelve-week-old C57BL/6 mice with segmental bone defect
Dosage 5 mg/kg
Formulation PBS
Administration Administered via i.p.
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000028715

Storage condition

Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. by MedKoo Biosciences, Inc.

Solubility

DMSO <1 mg/ml; Water 6 mg/ml by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
(25°C) * In vitro Water 3 mg/mL warming (5.96 mM); Ethanol100 mg/mL (198.89 mM); DMSO<1 mg/mL (<1 mM); In vivo 30% Propylene glycol, 5% Tween 80, 65% D5W30 mg/mL by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Plerixafor - Launched
Plerixafor Genzyme Corp Transplantation 2011/12/31 2012/11/1 Phase 4 Clinical
Plerixafor University of Florida Bone marrow transplantation 2011/4/30 2015/4/30 Phase 4 Clinical
Plerixafor Genzyme Corp Non-Hodgkin lymphoma 2010/10/31 2013/2/28 Phase 4 Clinical
Plerixafor Sanofi Non-Hodgkin lymphoma 2013/4/30 2014/4/30 Phase 3 Clinical
Plerixafor Case Comprehensive Cancer Center; Case Western Reserve University Multiple myeloma 2011/7/31 2013/6/30 Phase 3 Clinical
7

Safety Data of Plerixafor

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC USA
AbMole BioScience USA
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Apichem Chemical Technology Co., Ltd. China
Ark Pharm, Inc. USA
BOC Sciences 25mg/USD198(In stock)
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD76();50mg/USD199() USA
Cayman Chemical Company USA
MedChemexpress Co., Ltd. 10mg/USD76();50mg/USD199() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC 5mg/USD97(In stock);10mg/USD147(In stock);50mg/USD470(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD76();50mg/USD199() China
Taizhou Taifeng Chemical Co., Ltd. China
Target Molecule Corp. 10mg/USD60();25mg/USD116();50mg/USD198() USA
Wuhan Sunrise Technology Development Company Limited China
10

Related Products

Other Forms of 110078-46-1

Name CAS No Formula MW
Plerixafor (octahydrochloride) 155148-31-5 C28H62Cl8N8 794.47
(-)-56 1949801-52-8 C32H31F6N3O7 683.59
LDN 0088050 353484-30-7 C19H18BrNO2 372.26
TBID 1639895-85-4 C11H3Br4N3O2 528.78
TPI-1 79756-69-7 C12H6Cl2O2 253.08
PTP1B-IN-2 1919853-46-5 C34H36N2O9S2 680.79
C29 363600-92-4 C16H15NO4 285.29
BIPM 1070424-33-7 C23H22N2O3 374.43

Recommended Compounds in CXCR

Name CAS No Formula MW
AMD 3465 185991-24-6 C24H38N6 410.6
AMD 3465 185991-24-6 C24H38N6 410.5987
AZD8797 911715-90-7 C19H25N5OS2 403.5647
Baohuoside I 113558-15-9 C27H30O10 514.52
AMD-070 hydrochloride C21H30Cl3N5 458.86
WZ811 55778-02-4 C18H18N4 290.36
SRT3109 1204707-71-0 C18H23F2N5O4S2 475.53
UNBS5162 956590-23-1 C17H18N4O3 326.3498
NBI-74330 855527-92-3 C32H27F4N5O3 605.58
AMG 487 473719-41-4 C32H28F3N5O4 603.59
Reparixin (L-lysine salt) 266359-93-7 C20H35N3O5S 429.57
Reparixin 266359-83-5 C14H21NO3S 283.39
SCH 546738 906805-42-3 C23H31Cl2N7O 492.44
SCH 563705 473728-58-4 C23H27N3O5 425.48
SCH 527123 473727-83-2 C21H23N3O5 397.42
AMD-070 558447-26-0 C21H27N5 349.47
Plerixafor (octahydrochloride) 155148-31-5 C28H62Cl8N8 794.47
SRT3190 1204707-73-2 C18H23F2N5O4S2 475.53
Nicotinamide N-oxide 1986-81-8 C6H6N2O2 138.12404
AZD-5069 878385-84-3 C18H22F2N4O5S2 476.52

Recommended Compounds in Same Indication

Name CAS No Formula MW
CAL-101 870281-82-6 C22H18FN7O 415.42
PU-H71 873436-91-0 C18H21IN6O2S 512.37
Quisinostat 875320-29-9 C21H26N6O2 394.4702
AT9283 896466-04-9 C19H23N7O2 381.43
MLN9708 1239908-20-3 C20H23BCl2N2O9 517.12
Panobinostat 404950-80-7 C21H23N3O2 349.43
N-Hydroxy-3-(3-phenylsulfamoylphenyl)acrylamide 414864-00-9 C15H14N2O4S 318.34766
Carfilzomib 868540-17-4 C40H57N5O7 719.91
ARRY-520 (R enantiomer) 885060-08-2 C20H22F2N4O2S 420.48
ARRY-520 885060-09-3 C20H22F2N4O2S 420.48
Thalidomide 50-35-1 C13H10N2O4 258.23
Delanzomib 847499-27-8 C21H28BN3O5 413.28
RO4929097 847925-91-1 C22H20F5N3O3 469.4
Erastin 571203-78-6 C30H31ClN4O4 547.04
YM-155 781661-94-7 C20H19BrN4O3 443.29
AT7519 844442-38-2 C16H17Cl2N5O2 382.24
Danusertib 827318-97-8 C26H30N6O3 474.55
Masitinib 790299-79-5 C28H30N6OS 498.64
IC-87114 371242-69-2 C22H19N7O 397.43
Pralatrexate 146464-95-1 C23H23N7O5 477.47
11

Route of Synthesis

12

References

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More Information

Plerixafor

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