ChemicalBook
Chinese Japanese Germany Korea

PLERIXAFOR

Description In vitro In vivo
PLERIXAFOR
PLERIXAFOR structure
CAS No.
110078-46-1
Chemical Name:
PLERIXAFOR
Synonyms
AMD310;Mozobil;PLERIXAFOR;Sdz sid 791;Unii-S915p5499n;Plerixafor(AMD3100);AMD3100 (Plerixafor);Plerixafor/JM3100/AMD3100;1,4-bis((1,4,8,11-tetraazacyclotetradecan-1-yl)Methyl)benzene;1,4-Bis((1,4,8,11-tetraazacyclotetradecan-1-yl)Methyl)benzene,95+%
CBNumber:
CB11011749
Molecular Formula:
C28H54N8
Formula Weight:
502.791
MOL File:
110078-46-1.mol

PLERIXAFOR Properties

Melting point:
122-125°C
Density 
0.962
storage temp. 
Refrigerator
CAS DataBase Reference
110078-46-1
SAFETY
  • Risk and Safety Statements
HS Code  29339900

PLERIXAFOR Chemical Properties,Uses,Production

Description

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.

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. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7.

In vivo

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.

Description

Autologous hematopoietic stem cell (HSC) transplantation, a standard treatment for hematological malignancies, such as non-Hodgkin’s lymphoma or multiple myeloma, involves collection of HSCs from the patient, chemo- or radiotherapy of the patient to eliminate malignant cells, and retransplantation of the stored HSCs.
Plerixafor is a potent antagonist of the CXCR4 chemokine receptor and a first-in-class drug for stem cell mobilization. CXCR4 is specific for stromal-derived-factor-1 (SDF-1), a molecule endowed with potent chemotactic activity forlymphocytes. Because the interaction between SDF-1 and CXCR4 plays an important role in holding HSCs in the bone marrow, drugs that block the activity of CXCR4 receptor are capable of mobilizing HSCs into the bloodstream. In vitro, plerixafor potently blocks SDF-1 binding of CXCR4 and inhibits SDF-1-induced calcium flux (IC50 = 0.01-0.13 mg/mL) and chemotaxis (IC50 = 0.13 mg/mL) in several different cell types. Plerixafor, in combination with G-CSF, is specifically indicated to mobilize HSCs to the peripheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin’s lymphoma and multiple myeloma.

Chemical Properties

White Solid

Originator

AnorMED (Canada)

Uses

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively

Uses

Plerixafor is a hematopoietic stem cell (HSC) mobilizer that inhibits the CXCR4 chemokine receptor and blocks binding of its ligand, stromal cell-derived factor-1-α (SDF-1-α). on Dec. 15, 2008, as treatment in combination with granulocyte-colony stimulating factor (G-CSF) to mobilize HSCs to the peripheral blood for collection and subsequent autologous transplantation in p atients with non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM).

brand name

Mozobil

Side effects

The most common adverse reactions (occurring in more than 10% of patients) observed during plerixafor use include diarrhea, nausea, fatigue, injection-site reactions, headache, arthralgia, dizziness, and vomiting.

Chemical Synthesis

Plerixafor can be synthesized by several related procedures starting from tetraazacyclotetradecane, the macrocyclic tetraamine cyclam. The general synthetic strategy entails the masking of three of the four ring nitrogens, followed by alkylation with para-xylylene dibromide, and subsequent removal of the masking groups. In one approach, tetraazacyclotetradecane is protected as the phosphorotriamide derivative by reaction with tris (dimethylamino)phosphine followed by oxidation with carbon tetrachloride and sodium hydroxide. After condensation with xylylene dibromide, the dimeric bis-phosphoramide intermediate is hydrolyzed to plerixafor by treatment with dilute hydrochloric acid solution.

PLERIXAFOR Preparation Products And Raw materials

Raw materials

Preparation Products


PLERIXAFOR Suppliers

Global( 119)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 969 58
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21701 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24191 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29979 58
Chemwill Asia Co.,Ltd.
86-21-51086038
86-21-51861608 chemwill_asia@126.com;sales@chemwill.com;chemwill@hotmail.com;chemwill@gmail.com CHINA 23978 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 sales@jushengtech.com CHINA 28236 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 0 58

View Lastest Price from PLERIXAFOR manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-12-22 PLERIXAFOR
110078-46-1
US $1.00 / kg 1kg 98% 100KG career henan chemical co

110078-46-1(PLERIXAFOR)Related Search:


Copyright 2017 © ChemicalBook. All rights reserved