Plerixafor(AMD3100)

Plerixafor(AMD3100) - Names and Identifiers

Name	PLERIXAFOR
Synonyms	Mozobil PLERIXAFOR Sdz sid 791 Unii-S915p5499n Plerixafor(AMD3100) MSC1936369B, SAR 245509 1,4-Bis((1,4,8,11-Tetraazacyclotetradecan-1-Yl)Methyl)Benzene 1,1'-[1,4-Phenylenebis(methylene)]bis-1,4,8,11-tetraazacyclotetradecane 1,4,8,11-Tetraazacyclotetradecane, 1,1'-(1,4-phenylenebis(methylene))bis- 1,1'-(benzene-1,4-diyldimethanediyl)bis(1,4,8,11-tetraazacyclotetradecane) 1-[[4-(1,4,8,11-tetrazacyclotetradec-1-ylmethyl)phenyl]methyl]-1,4,8,11-tetrazacyclotetradecane 1,1'-[1,4-Phenylenebis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane]Octahydrobromide Dihydrate 1-{[4-(1,4,8,11-tetraazacyclotetradecan-1-ylMethyl)phenyl]Methyl}-1,4,8,11-tetraazacyclotetradecane 1,1'-(benzene-1,4-diyldimethanediyl)bis-1,4,8,11-tetraazacyclotetradecane octahydrobromide dihydrate
CAS	110078-46-1 155148-32-6
EINECS	1592732-453-0
InChI	InChI=1/C28H54N8.8BrH.2H2O/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;81H;21H2

Plerixafor(AMD3100) - Physico-chemical Properties

Molecular Formula	C28H54N8
Molar Mass	502.78
Density	0.962
Melting Point	122-125°C
Boling Point	657.5±55.0 °C(Predicted)
Flash Point	497°C
Solubility	Methanol (Slightly), Water (Slightly)
Vapor Presure	1.06E-34mmHg at 25°C
Appearance	Solid
Color	White to Pale Beige
pKa	10.60±0.20(Predicted)
Storage Condition	Keep in dark place,Inert atmosphere,2-8°C
Stability	Hygroscopic
Sensitive	IRRITANT
MDL	MFCD16621081
In vitro study	Plerixafor inhibits cxcl12-mediated chemotaxis with slightly higher potency than its affinity for CXCR4. Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibited SDF-1-mediated GTP-binding, SDF-1-mediated calcium ion flux, and SDF-1-stimulated chemotaxis with IC50 of 27 nM,572 nM, and 51 nM, respectively. When stimulated with their cognate ligands, Plerixafor did not inhibit calcium flux in cells expressing CXCR3,CCR1,CCR2b,CCR4,CCR5, or CCR7, nor did Plerixafor inhibit LTB4 receptor binding. Plerixafor by itself does not induce calcium ion flux in CCRF-CEM cells expressing multiple GPCRs, including CXCR4,CCR4, and ccr7.
In vivo study	In diabetic mice, Plerixafor single-dose topical administration promotes wound healing by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing fibroblasts and monocytes/macrophages, thereby increasing angiogenesis and angiogenesis play a role. Congener mice were administered PBS,IGF1,PDGF,SCF, or VEGF for 5 consecutive days, and Plerixafor was administered on day 5. Compared with the test groups of PDGF,SCF and VEGF combined with Plerixafor, the number and size of colonies were the highest in the injected mice of IGF1 plus Plerixafor.

Plerixafor(AMD3100) - Risk and Safety

HS Code

29339900

Plerixafor(AMD3100) - Introduction

Proxafu (Plerixafor) is a small molecule chemokine receptor CXCR4 blocker and blocks the binding of its homologous ligand stromal cell-derived factor -1 α(SDF-1α). SDF-1α and CXCR4 are thought to play a role in the transplantation and return of human hematopoietic stem cells (HSCs) to the bone marrow cavity. Once in the bone marrow, the stem cells CXCR4 can anchor these cells to the bone marrow stroma, directly through SDF-1α or induce other adhesion molecules. plerixafor treatment resulted in leukocytosis and elevation of circulating hematopoietic progenitor cells in mice, dogs and humans. plerixafor-driven CD34 + cells can have up to one year of regeneration in canine transplantation models

indications

Combined treatment with G-CSF for non-Hodgkin's lymphoma and multiple myeloma after autologous stem cell transplantation.

adverse reactions

the most common adverse reactions (≥ 10%): diarrhea, nausea, fatigue, local injection reaction, headache, arthralgia, dizziness and vomiting.

biological activity

Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist that acts on CXCR4 and CXCL12-mediated chemotaxis. IC50 in cell-free tests is 44 nM and 5.7 nM respectively. Plerixafor can inhibit human immunodeficiency virus (HIV) replication.

Last Update：2024-04-10 22:29:15

Plerixafor(AMD3100) - Nature

melting point	122-125°C
boiling point	657.5±55.0 °C(Predicted)
density	0.962
storage conditions	Keep in dark place,Inert atmosphere,2-8°C
acidity coefficient (pKa)	10.60±0.20(Predicted)

Last Update：2024-04-10 22:41:03

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