Plerixafor (Synonyms: 普乐沙福; AMD 3100; JM3100; SID791)

目录号: HY-10046 纯度: 99.90%: Data Sheet SDS COA 产品使用指南
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Plerixafor (AMD 3100) 是选择性的 CXCR4 拮抗剂，IC₅₀ 为 44 nM。Plerixafor 是一种免疫刺激剂和造血干细胞动员剂，也是 CXCR7 的变构激动剂。Plerixafor 抑制 HIV-1 和 HIV-2 的复制，EC₅₀ 为 1-10 nM。

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Plerixafor Chemical Structure

CAS No. : 110078-46-1

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Other Forms of Plerixafor:

MCE 顾客使用本产品发表的 97 篇科研文献

RT-PCR

Proliferation Assay

IHC

: Plerixafor purchased from MCE. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944. [Abstract]; Viability of cells treated with combinations different concentrations of AMD3100 and Olaparib for 24 h.

: Plerixafor purchased from MCE. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944. [Abstract]; Immunohistochemical staining of proliferation-related protein, Ki-67, in breast cancer after treatment with control, AMD3100 (2.5 mg/kg), Olaparib, or a combination of AMD3100 and Olaparib.

: Plerixafor purchased from MCE. Usage Cited in: Cell Death Dis. 2022 Feb 4;13(2):118. [Abstract]; PGK1 induced the CXCR4-mediated phosphorylation of AKT (p-AKT) and ERK (p-ERK), and blockade of CXCR4 signaling by AMD3100 (48 h) treatment did not alter cellular PGK1 expression in KIRC cells.

: Plerixafor purchased from MCE. Usage Cited in: Bioact Mater. 2021 Jan 7;6(7):2039-2057. [Abstract]; Western blot analysis of the expression of CXCR4, integrin αvβ3, p-Jak2, Jak2, p-FAK, FAK, p-STAT3 and STAT3 in MSCs (pretreated with a CXCR4 inhibitor (AMD3100; 20 μM; pretreated with 1 h) and an integrin αvβ3 inhibitor (cyclo(-RGDfK))) after the addition of 152RM for 24 h.

: Plerixafor purchased from MCE. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633. [Abstract]; Transwell assays indicated that AMD3100 treatment (1 µg/ml, 24 hours) significantly decreases the migration and invasion of Caco-2-HOXB5 cells.

: Plerixafor purchased from MCE. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633. [Abstract]; Caco-2 cells are incubated with vehicle or AMD3100 (1 µg/ml, 24 hours) after lentivirus transfection (LV-HOXB5), then Western blotting assays are conducted to measure the protein levels of CXCL12, HOXB5, CXCR4, p-ERK and p-ETS1 in the indicated cell lines.

: Plerixafor purchased from MCE. Usage Cited in: Adv Funct Mater. 2020, 2000309.; NOD/SCID mice were i.p. injected with AMD3100 (4 mg/kg). After 1 h, the mice are i.v. injected with iFluor 647-labeled Aazo@CMSN. At 12 h after nanoparticle injection, the mouse craniums are excised for the observation of nanoparticle bone marrow niches targeting under CLSM. Pre-treatment with AMD3100 significantly declined the bone marrow niches targeting of the nanoparticles.

: Plerixafor purchased from MCE. Usage Cited in: Cell Mol Immunol. 2020 Mar;17(3):283-299. [Abstract]; ELISA of IL-1β in supernatants of BV2 cells stimulated with gp120 LAV (0.5 μg/mL) for 24 h in the presence of increasing doses of a CXCR4-specific inhibitor (AMD3100, 0.1-10 μM; prestimulated with 30 min-2 h).

: Plerixafor purchased from MCE. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037. [Abstract]; Additional EMT-related proteins (Snail and Slug) are downregulated by AMD3100 (5 mg/kg or 3.5 mg/kg) in tumor samples from both diet groups, as quantified by immunoblotting.

: Plerixafor purchased from MCE. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037. [Abstract]; IF staining of the tumor tissue sections showed decreased Ki67 and a reversal of EMT markers indicated by increased E-cadherin and decreased N-cadherin expression in the AMD3100 (5 mg/kg or 3.5 mg/kg) treated groups.

: Plerixafor purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(3):890-906. [Abstract]; The protein expression of LRRC4, SDF-1, CXCR4, ERK, Slit2 and VEGF in the brain tissue of rats is determined by Western blotting.

: Plerixafor purchased from MCE. Usage Cited in: Int J Biol Sci. 2017 May 5;13(5):604-614. [Abstract]; Epithelial cells with or without AMD3100 pretreatment are cultured in conditioned medium (CM) from LPS-treated NFs or LTA-treated NFs for 3 days, and the secretion of TNF-α in the supernatant of culture is detected by ELISA. Epithelial cells cultured in MSM are used as control. Both LPS-treated NFs and LTA-treated NFs enhanced the section of TNF-α by epithelial cells compared with control. Pretreatment of epithelial cells with AMD3100 significantly attenuates the increase of TNF-α.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM^[1]^[2]^[3]^[4]^[7].

IC₅₀ & Target^[3]^[7]

¹²⁵I-CXCL12-CXCR4

44 nM (IC₅₀)

¹²⁵I-CXCL12-CXCR7

HIV-1

1-10 nM (EC₅₀)

HIV-2

1-10 nM (EC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	245 nM Compound: AMD-3100	Displacement of [125I]CXCL12 from CXCR4 in human CEM cells Displacement of [125I]CXCL12 from CXCR4 in human CEM cells	[PMID: 19053768]
CEM-SS	CC₅₀	> 10 μM Compound: AMD-3100	Concentration of compound causing 50% death of uninfected cells Concentration of compound causing 50% death of uninfected cells	[PMID: 14698189]
CEM-SS	CC₅₀	> 5 μM Compound: AMD-3100	Cytotoxicity against human CEM-SS cells by MTT assay Cytotoxicity against human CEM-SS cells by MTT assay	[PMID: 19356827]
CEM-SS	EC₅₀	0.127 μM Compound: AMD-3100	Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells	[PMID: 14698189]
CEM-SS	IC₅₀	0.32 μM Compound: AMD-3100	Antiviral activity against HIV1 LAI in human CEM-SS cells assessed as inhibition of viral replication Antiviral activity against HIV1 LAI in human CEM-SS cells assessed as inhibition of viral replication	[PMID: 19356827]
CHO	IC₅₀	0.051 μM Compound: AMD3100	Competitive binding affinity to CXCR4 receptor (unknown origin) expressed in CHO cells incubated for 40 mins by 12G5 antibody based fluorescence analysis Competitive binding affinity to CXCR4 receptor (unknown origin) expressed in CHO cells incubated for 40 mins by 12G5 antibody based fluorescence analysis	[PMID: 30978562]
CHO	IC₅₀	65 nM Compound: AMD3100	Binding affinity to CXCR4 (unknown origin) expressed in CHO cells measured after 40 mins by 12G5 antibody competition assay Binding affinity to CXCR4 (unknown origin) expressed in CHO cells measured after 40 mins by 12G5 antibody competition assay	[PMID: 27658790]
CHO-K1	IC₅₀	0.04 nM Compound: AMD-3100	Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells	[PMID: 17715128]
CHO-K1	IC₅₀	0.09 nM Compound: AMD-3100	Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells	[PMID: 17715128]
CHO-K1	IC₅₀	0.81 nM Compound: AMD-3100	Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells	[PMID: 17715128]
GHOST CCR5	IC₅₀	> 5 μM Compound: AMD-3100	Inhibitory concentration of compound against HIV-1 Ba1 strain in GHOST CCR5 cell line Inhibitory concentration of compound against HIV-1 Ba1 strain in GHOST CCR5 cell line	[PMID: 14698189]
GHOST CXCR4	IC₅₀	0.00095 μM Compound: AMD-3100	Inhibitory concentration of compound against HIV-1 LAI strain in GHOST CXCR4 cell line Inhibitory concentration of compound against HIV-1 LAI strain in GHOST CXCR4 cell line	[PMID: 14698189]
HEK293	IC₅₀	143.7 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	175.3 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	196.6 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	2.3 nM Compound: AMD-3100	Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	213.1 nM Compound: 1; AMD3100	Displacement of [125I]CXCL12 from human CXCR4 expressed in HEK293 cell membranes after 1.5 hrs by Topcount method Displacement of [125I]CXCL12 from human CXCR4 expressed in HEK293 cell membranes after 1.5 hrs by Topcount method	[PMID: 29314840]
HEK293	IC₅₀	235.6 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	258.5 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 V99A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 V99A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	259 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	265.8 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 I284A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 I284A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	289.1 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	296.4 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 H113A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 H113A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	300.2 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	4.6 nM Compound: AMD-3100	Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	469.5 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 E277A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 E277A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	5.3 nM Compound: AMD-3100	Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	6.2 nM Compound: AMD-3100	Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	7 nM Compound: AMD-3100	Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	72.7 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	9 nM Compound: AMD-3100	Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	9.2 nM Compound: AMD-3100	Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days	[PMID: 19451305]
HEK293	IC₅₀	> 1000 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 D171A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 D171A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	> 1000 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 D262A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 D262A mutant expressed in HEK293 cells	[PMID: 19451305]
HEK293	IC₅₀	> 1000 nM Compound: AMD-3100	Inhibition of Mab 12G5 binding to CXCR4 E288A/L290A mutant expressed in HEK293 cells Inhibition of Mab 12G5 binding to CXCR4 E288A/L290A mutant expressed in HEK293 cells	[PMID: 19451305]
HL-60	IC₅₀	15.2 μM Compound: 1, AMD-3100	Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells	[PMID: 19188071]
HuT78	CC₅₀	241 μM Compound: 1	Cellular cytotoxicity against HUT-78 cells. Cellular cytotoxicity against HUT-78 cells.	[PMID: 7562918]
Jurkat	IC₅₀	27.4 nM Compound: 1, AMD-3100	Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration	[PMID: 19188071]
MT4	CC₅₀	50 μM Compound: 37	Concentration required to cause 50% death of uninfected MT-4 cells Concentration required to cause 50% death of uninfected MT-4 cells	[PMID: 9925728]
MT4	CC₅₀	6.5 μM Compound: AMD-3100	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 19356827]
MT4	CC₅₀	> 10 μM Compound: AMD-3100	Concentration of compound causing 50% death of uninfected cells Concentration of compound causing 50% death of uninfected cells	[PMID: 14698189]
MT4	CC₅₀	> 10 μg/mL Compound: AMD-3100	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 23157587]
MT4	CC₅₀	> 421 μM Compound: 1, AMD-3100	Cytotoxicity against human MT4 cells after 4 days by MTT method Cytotoxicity against human MT4 cells after 4 days by MTT method	[PMID: 20043638]
MT4	CC₅₀	> 421 μM Compound: 10d	Concentration required to reduce the viability of mock infected cells by 50% Concentration required to reduce the viability of mock infected cells by 50%	[PMID: 8568797]
MT4	CC₅₀	> 50 μM Compound: AMD3100	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 26094944]
MT4	CC₅₀	> 50 μM Compound: AMD3100	Cytotoxicity against human MT4 cells by MTT assay in presence of 10 uM of chloroquine Cytotoxicity against human MT4 cells by MTT assay in presence of 10 uM of chloroquine	[PMID: 26094944]
MT4	CC₅₀	> 50 μM Compound: AMD3100	Cytotoxicity against human MT4 cells by MTT assay in presence of 2.5 uM of chloroquine Cytotoxicity against human MT4 cells by MTT assay in presence of 2.5 uM of chloroquine	[PMID: 26094944]
MT4	CC₅₀	> 50 μM Compound: AMD3100	Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine	[PMID: 26094944]
MT4	CC₅₀	> 50 μM Compound: AMD3100	Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	[PMID: 32305183]
MT4	CC₅₀	> 50 μM Compound: AMD3100	Cytotoxicity against in human MT-4 after 5 days by MTT assay Cytotoxicity against in human MT-4 after 5 days by MTT assay	[PMID: 33316719]
MT4	EC₅₀	0.004 μM Compound: 1, AMD-3100	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay	[PMID: 20043638]
MT4	EC₅₀	0.0042 μM Compound: 10d	Effective concentration against HIV-1(IIIB) replication in MT-4 cells Effective concentration against HIV-1(IIIB) replication in MT-4 cells	[PMID: 8568797]
MT4	EC₅₀	0.0059 μM Compound: 10d	Effective concentration against HIV-2(ROD) replication in MT-4 cells Effective concentration against HIV-2(ROD) replication in MT-4 cells	[PMID: 8568797]
MT4	EC₅₀	0.008 μM Compound: AMD3100	Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.008 μM Compound: AMD3100	Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.008 μM Compound: AMD3100	Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.014 μM Compound: AMD3100	Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.025 μM Compound: AMD3100	Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine	[PMID: 26094944]
MT4	EC₅₀	0.028 μM Compound: AMD3100	Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.032 μM Compound: AMD3100	Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay	[PMID: 26094944]
MT4	EC₅₀	0.034 μM Compound: AMD3100	Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.039 μM Compound: AMD3100	Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 2.5 uM of chloroquine Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 2.5 uM of chloroquine	[PMID: 26094944]
MT4	EC₅₀	0.049 μM Compound: AMD3100	Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.056 μM Compound: AMD3100	Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.065 μM Compound: AMD-3100	Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells	[PMID: 14698189]
MT4	EC₅₀	10 μM Compound: 37	Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells	[PMID: 9925728]
MT4	EC₅₀	2 nM Compound: AMD3100; 15c; 16c	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 26974376]
MT4	EC₅₀	2 nM Compound: AMD3100; 15c; 16c	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 26974376]
MT4	IC₅₀	0.017 μg/mL Compound: AMD-3100	Antiviral activity against X4 HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of viral replication pre-incubated for 30 mins measured 5 days post infection by MTT assay Antiviral activity against X4 HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of viral replication pre-incubated for 30 mins measured 5 days post infection by MTT assay	[PMID: 23157587]
MT4	IC₅₀	0.41 μM Compound: AMD-3100	Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral replication Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral replication	[PMID: 19356827]
MT4	IC₅₀	1.5 ng/mL Compound: AMD-3100	Antiviral activity against HIV1 NL4.3 in human MT4 cells Antiviral activity against HIV1 NL4.3 in human MT4 cells	[PMID: 17452489]
PBMC	CC₅₀	> 10 μM Compound: 1a, AMD-3100	Cytotoxicity against PBMC Cytotoxicity against PBMC	[PMID: 17000109]
PBMC	CC₅₀	> 10 μM Compound: AMD-3100	Concentration of compound causing 50% death of uninfected cells Concentration of compound causing 50% death of uninfected cells	[PMID: 14698189]
PBMC	CC₅₀	> 10 μg/mL Compound: AMD-3100	Cytotoxicity against human PBMC cells by MTT assay Cytotoxicity against human PBMC cells by MTT assay	[PMID: 23157587]
PBMC	EC₅₀	0.0038 μM Compound: AMD-3100	Effective concentration of compound against HIV-1 89.6 strain in PBMC cells Effective concentration of compound against HIV-1 89.6 strain in PBMC cells	[PMID: 14698189]

体外研究
(In Vitro)

CXCR4 抑制剂 Plerixafor (AMD3100) 是一种有效的 CXCL12 介导的趋化性抑制剂 (IC₅₀，5.7 nM)，效力略优于其对 CXCR4 的亲和力。Plerixafor 干扰 CXCR4 与其天然配体 SDF-1 (CXCL12) 的相互作用。用 CCX771 或 CXCL11 处理细胞对 CXCL12 介导的 MOLT-4 或 U937 TEM 没有影响。相反，10 μM Plerixafor 在两种细胞系中抑制 CXCL12 介导的 TEM^[1]。
Plerixafor 可防止肿瘤相关巨噬细胞 (TAM) 浸润到肿瘤组织中^[8]。

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

体内研究
(In Vivo)

Plerixafor (2 mg/kg) 对 UUO 小鼠给药会加剧肾间质 T 细胞浸润，导致促炎细胞因子 IL-6 和 IFN-γ 的产生增加，并降低抗炎细胞因子 IL-10 的表达^[5]。
CXCR4 拮抗剂 Plerixafor (AMD3100) 在 8 周时显著减少了血管周围和间质纤维化^[6]。LD50，小鼠，SC：16.3 mg/kg；LD50，大鼠，SC：>50 mg/kg；LD50，小鼠和大鼠，静脉注射：5.2 mg/kg^[5]。

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

Clinical Trial

分子量

502.78

Formula

C₂₈H₅₄N₈

CAS 号

110078-46-1

性状

固体

颜色

White to off-white

中文名称

普乐沙福

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

Ethanol 中的溶解度 : 50 mg/mL (99.45 mM; 超声助溶)

DMSO 中的溶解度 : 1.92 mg/mL (3.82 mM; ultrasonic and warming and adjust pH to 7 with 1 M HCL and heat to 60°C; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9889 mL	9.9447 mL	19.8894 mL
5 mM	0.3978 mL	1.9889 mL	3.9779 mL
10 mM	0.1989 mL	0.9945 mL	1.9889 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.97 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.97 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.97 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.90%

选择批次：

Data Sheet (646 KB) SDS (393 KB)

COA (285 KB) HNMR (252 KB) RP-HPLC (206 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Yang J, et al. Continuous AMD3100 Treatment Worsens Renal Fibrosis through Regulation of Bone Marrow Derived Pro-Angiogenic Cells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926. [Content Brief]

[2]. Seki JT, et al. Chemical Stability of Plerixafor after Opening of Single-Use Vial. Can J Hosp Pharm. 2017 Jul-Aug;70(4):270-275. [Content Brief]

[3]. Zabel BA, et al. 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. [Content Brief]

[4]. De Clercq E, et al. Mozobil® (Plerixafor, AMD3100), 10 years after its approval by the US Food and Drug Administration. Antivir Chem Chemother. 2019 Jan-Dec;27:2040206619829382. [Content Brief]

[5]. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55. [Content Brief]

[6]. Chu PY, et al. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616. [Content Brief]

[7]. Schols D, et al. HIV co-receptor inhibitors as novel class of anti-HIV drugs. Antiviral Res. 2006 Sep;71(2-3):216-26. [Content Brief]

[8]. Zheng J, et al. Toward Normalization of the Tumor Microenvironment for Cancer Therapy. Integr Cancer Ther. 2019;18:1534735419862352. [Content Brief]

Cell Assay ^[2]	U87MG cells are seeded in 96-well plates at the density of 6×10³ cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]^[4]	Mice^[3] Male C57bl/6 mice (6-7 weeks old, weighing 20 g) are used. The animals are acclimated to the housing environment, which is SPF and had a temperature of 22°C and a 12h/12h light/dark cycle for a week. Then, they are randomly divided into following experimental groups, with 8 mice in each group: normal (no specific intervention), UUO+AMD3100 (mice received UUO surgery and 2 mg/kg AMD3100), and UUO+PBS (mice received UUO surgery and the same volume of PBS). AMD3100 and PBS are administered via intraperitoneal injection every day until sacrifice. Rats^[4] The CXCR4 antagonist, AMD3100 dissolved in H₂O, is delivered in the type 2 diabetic sand rat model at a dose of 6 mg/kg per day for 8 weeks. In complementary studies, the effect of CXCR4 antagonism (AMD3100 6mg/kg/d) on regulatory T cell numbers is examined. For these studies, AMD3100 or vehicle is delivered via minipump for a period of one week. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Yang J, et al. Continuous AMD3100 Treatment Worsens Renal Fibrosis through Regulation of Bone Marrow Derived Pro-Angiogenic Cells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926. [Content Brief] [2]. Seki JT, et al. Chemical Stability of Plerixafor after Opening of Single-Use Vial. Can J Hosp Pharm. 2017 Jul-Aug;70(4):270-275. [Content Brief] [3]. Zabel BA, et al. 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. [Content Brief] [4]. De Clercq E, et al. Mozobil® (Plerixafor, AMD3100), 10 years after its approval by the US Food and Drug Administration. Antivir Chem Chemother. 2019 Jan-Dec;27:2040206619829382. [Content Brief] [5]. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55. [Content Brief] [6]. Chu PY, et al. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616. [Content Brief] [7]. Schols D, et al. HIV co-receptor inhibitors as novel class of anti-HIV drugs. Antiviral Res. 2006 Sep;71(2-3):216-26. [Content Brief] [8]. Zheng J, et al. Toward Normalization of the Tumor Microenvironment for Cancer Therapy. Integr Cancer Ther. 2019;18:1534735419862352. [Content Brief]

Plerixafor 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	1.9889 mL	9.9447 mL	19.8894 mL	49.7235 mL
Ethanol	5 mM	0.3978 mL	1.9889 mL	3.9779 mL	9.9447 mL
	10 mM	0.1989 mL	0.9945 mL	1.9889 mL	4.9724 mL
	15 mM	0.1326 mL	0.6630 mL	1.3260 mL	3.3149 mL
	20 mM	0.0994 mL	0.4972 mL	0.9945 mL	2.4862 mL
	25 mM	0.0796 mL	0.3978 mL	0.7956 mL	1.9889 mL
	30 mM	0.0663 mL	0.3315 mL	0.6630 mL	1.6575 mL
	40 mM	0.0497 mL	0.2486 mL	0.4972 mL	1.2431 mL
	50 mM	0.0398 mL	0.1989 mL	0.3978 mL	0.9945 mL
	60 mM	0.0331 mL	0.1657 mL	0.3315 mL	0.8287 mL
	80 mM	0.0249 mL	0.1243 mL	0.2486 mL	0.6215 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Plerixafor (Synonyms: 普乐沙福; AMD 3100; JM3100; SID791)

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Plerixafor (Synonyms: 普乐沙福; AMD 3100; JM3100; SID791)

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Other Forms of Plerixafor:

Plerixafor 相关抗体

MCE 顾客使用本产品发表的 97 篇科研文献

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