Description In vitro In vivo
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PLERIXAFOR

Description In vitro In vivo
Product Name
PLERIXAFOR
CAS No.
110078-46-1
Chemical Name
PLERIXAFOR
Synonyms
AMD310;CS-269;Mozobil;AMD-3329;Plerixafo;PLERIXAFOR;Sdz sid 791;Unii-S915p5499n;MOZOBIL PLERIXAFOR;Plerixafor(AMD3100)
CBNumber
CB11011749
Molecular Formula
C28H54N8
Formula Weight
502.78
MOL File
110078-46-1.mol
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PLERIXAFOR Property

Melting point:
122-125°C
Boiling point:
657.5±55.0 °C(Predicted)
Density 
0.962
storage temp. 
Keep in dark place,Inert atmosphere,2-8°C
solubility 
Methanol (Slightly), Water (Slightly)
form 
Solid
pka
10.60±0.20(Predicted)
color 
White to Pale Beige
Stability:
Hygroscopic
CAS DataBase Reference
110078-46-1
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Safety

HS Code 
29339900
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

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N-Bromosuccinimide Price

TCI Chemical
Product number
P2678
Product name
Plerixafor
Packaging
50MG
Price
$99
Updated
2024/03/01
TCI Chemical
Product number
P2678
Product name
Plerixafor
Packaging
250MG
Price
$297
Updated
2024/03/01
TRC
Product number
P580500
Product name
Plerixafor
Packaging
5mg
Price
$80
Updated
2021/12/16
TRC
Product number
P580500
Product name
Plerixafor
Packaging
50mg
Price
$350
Updated
2021/12/16
Usbiological
Product number
019844
Product name
Plerixafor
Packaging
10mg
Price
$403
Updated
2021/12/16
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PLERIXAFOR Chemical Properties,Usage,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 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). This agent was approved 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 patients with non-Hodgkin''s lymphoma (NHL) and multiple myeloma (MM). Selective CXCR4 antagonist.

Uses

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

Definition

ChEBI: Plerixafor is an azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma. It has a role as an immunological adjuvant, an antineoplastic agent, an anti-HIV agent and a C-X-C chemokine receptor type 4 antagonist. It is an azamacrocycle, a crown amine, a secondary amino compound, an azacycloalkane, a tertiary amino compound and a member of benzenes. It is functionally related to a 1,4,8,11-tetraazacyclotetradecane.

brand name

Mozobil

Clinical Use

Chemokine receptor antagonist:

To enhance mobilisation of haematopoietic stem cells to the peripheral blood for collection and subsequent autologous transplantation in patients with lymphoma and multiple myeloma whose cells mobilise poorly

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.

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.

Metabolism

Not metabolised.
About 70% of a dose is eliminated in the urine within 24 hours.

References

[1]zabel ba, wang y, lewén s, berahovich rd, penfold me, zhang p, powers j, summers bc, miao z, zhao b, jalili a, janowska-wieczorek a, jaen jc, schall tj. 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.
[2].li j, oupicky d. effect of biodegradability on cxcr4 antagonism, transfection efficacy and antimetastatic activity of polymeric plerixafor.biomaterials. 2014 jul;35(21):5572-9.
[3]. broxmeyer he. chemokines in hematopoiesis. curr opin hematol. 2008 jan;15(1):49-58.
[4]. devi s, wang y, chew wk, lima r, a-gonzález n, mattar cn, chong sz, schlitzer a, bakocevic n, chew s, keeble jl, goh cc, li jl, evrard m, malleret b, larbi a, renia l, haniffa m, tan sm, chan jk, balabanian k, nagasawa t, bachelerie f, hidalgo a, ginhoux f, kubes p, ng lg. neutrophil mobilization via plerixafor-mediated cxcr4 inhibition arises from lung demargination and blockade of neutrophil homing to the bone marrow. j exp med. 2013 oct 21;210(11):2321-36.
[5]. mcdermott dh, liu q, velez d, lopez l, anaya-o'brien s, ulrick j, kwatemaa n, starling j, fleisher ta, priel da, merideth ma, giuntoli rl, evbuomwan mo, littel p, marquesen mm, hilligoss d, decastro r, grimes gj, hwang st, pittaluga s, calvo kr, stratton p, cowen ew, kuhns db, malech hl, murphy pm. a phase 1

PLERIXAFOR Preparation Products And Raw materials

Raw materials

Preparation Products

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PLERIXAFOR Suppliers

Hubei Changrun Biomedical Technology Co., Ltd.
Tel
027-63496417 13007129042
Fax
13476107660
Email
3294393103@qq.com
Country
China
ProdList
296
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58
Wuhan Yingnuo Pharmaceutical Technology Co., Ltd.
Tel
+86-027-59232304 15387063101
Email
2881924050@qq.com
Country
China
ProdList
9989
Advantage
58
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8014
Advantage
62
Shanghai jerryxing Biomedical Technology Co., Ltd
Tel
17721492509
Email
643638326@qq.com
Country
China
ProdList
5345
Advantage
58
Wuhan Sunrise Technology Development Co., Ltd.
Tel
27-027-83314682 13554138826
Fax
+86 (27) 8331-4682
Email
whsrtech@vip.163.com
Country
China
ProdList
219
Advantage
62
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chemvon Biotechnology Co., Ltd
Tel
021-50790412
Fax
+86-21-50790419
Email
info@chemvon.com
Country
China
ProdList
371
Advantage
57
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Fax
86-021-50426522,50426273
Email
sales@jingyan-chemical.com
Country
China
ProdList
9976
Advantage
60
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View Lastest Price from PLERIXAFOR manufacturers

Wuhan Boye Science And Technology Development Co., Ltd.
Product
Plerixafor 110078-46-1
Price
US $921.60/g/Bag
Min. Order
1g
Purity
99%
Supply Ability
5KG
Release date
2021-03-23
Anhui Ruihan Technology Co., Ltd
Product
Plerixafor 110078-46-1
Price
US $50.00/kg
Min. Order
1kg
Purity
99.9%
Supply Ability
10000tons
Release date
2023-08-22
Hebei Ruiyao Biotechnology Co. Ltd
Product
PLERIXAFOR 110078-46-1
Price
US $10.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
1000kg
Release date
2023-08-02

110078-46-1, PLERIXAFORRelated Search:


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