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AMD3100 (Plerixafor) CXCR4 길항제

Name: AMD3100 (Plerixafor)
Brand: Selleck Chemicals
SKU: S8030
Rating: 5 (110 reviews)

제품 번호S8030

Plerixafor (AMD3100, JM 3100, SID791)는 무세포 분석에서 각각 44 nM 및 5.7 nM의 IC50을 갖는 CXCR4 및 CXCL12 매개 화학주성용 케모카인 수용체 길항제입니다. Plerixafor는 human immunodeficiency virus (HIV) 복제를 억제합니다.

AMD3100 (Plerixafor) CXCR 길항제 Chemical Structure

화학 구조

분자량: 502.78

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품질 관리

배치: 순도: 99.93%

99.93

관련 타겟	Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas GPR
기타 CXCR 억제제	AZD5069 SB 225002 Reparixin (Repertaxin) WZ811 Navarixin (SCH-527123) LIT-927 AMG 487 SX-682 LY2510924 Danirixin (GSK1325756)

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
CHOK1	Function assay			Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells, IC50 = 0.00004 μM.	17715128
CHOK1	Function assay			Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells, IC50 = 0.00009 μM.	17715128
CHOK1	Function assay			Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50 = 0.00081 μM.	17715128
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0019 μM.	17599916
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0019 μM.	17599916
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50 = 0.002 μM.	26974376
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50 = 0.002 μM.	26974376
HEK293	Antiviral assay		2 days	Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0023 μM.	19451305
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0024 μM.	17599916
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.003 μM.	17599916
PBMC	Function assay			Effective concentration of compound against HIV-1 89.6 strain in PBMC cells, EC50 = 0.0038 μM.	14698189
MT4	Antiviral assay		4 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay, EC50 = 0.004 μM.	20043638
MT-4	Function assay			Effective concentration against HIV-1(IIIB) replication in MT-4 cells, EC50 = 0.0042 μM.	8568797
HEK293	Antiviral assay		2 days	Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0046 μM.	19451305
HEK293	Antiviral assay		2 days	Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0053 μM.	19451305
MT-4	Function assay			Effective concentration against HIV-2(ROD) replication in MT-4 cells, EC50 = 0.0059 μM.	8568797
CEM-CCRF	Function assay		30 mins	Inhibition of PE-conjugated-12G5 anti-CXCR4 antibody binding to CXCR4 in human CEM-CCRF cells preincubated for 30 mins followed by antibody addition by FACS Canto II cytofluorometric analysis, IC50 = 0.006 μM.	27571038
HEK293	Antiviral assay		2 days	Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0062 μM.	19451305
HEK293	Antiviral assay		2 days	Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.007 μM.	19451305
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.0076 μM.	17599916
MT-4	Antiviral assay			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, EC50 = 0.008 μM.	18378713
MT-4	Antiviral assay			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, EC50 = 0.008 μM.	18378713
MT-4	Antiviral 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 after 20 passages selected in presence of compound, EC50 = 0.008 μM.	18378713
HEK293	Antiviral assay		2 days	Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.009 μM.	19451305
HEK293	Antiviral assay		2 days	Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0092 μM.	19451305
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.014 μM.	17599916
MT-4	Antiviral 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, EC50 = 0.014 μM.	18378713
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.017 μM.	17599916
CD4+ T	Function assay			Antagonist activity at CXCR4 in human CD4+ T cells assessed as inhibition of CXCL12-mediated cytosolic calcium level preincubated with compounds followed by CXCL12 stimulation by calcium 4 dye-based FLIPR assay, IC50 = 0.018 μM.	29494843
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.019 μM.	17599916
MT4	Antiviral assay		5 days	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, EC50 = 0.025 μM.	26094944
Jurkat	Function assay			Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration, IC50 = 0.0274 μM.	19188071
MT-4	Antiviral assay			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, EC50 = 0.028 μM.	18378713
MT4	Antiviral assay		5 days	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, EC50 = 0.032 μM.	26094944
MT-4	Antiviral assay			Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.034 μM.	18378713
MT4	Antiviral assay		5 days	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, EC50 = 0.039 μM.	26094944
U87.CD4	Antiviral assay			Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.046 μM.	17599916
MT-4	Antiviral assay			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, EC50 = 0.049 μM.	18378713
MT-4	Antiviral assay			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, EC50 = 0.056 μM.	18378713
MT-4	Function assay			Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells, EC50 = 0.065 μM.	14698189
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells, IC50 = 0.0727 μM.	19451305
IR983F	Function assay			Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells, IC50 = 0.108 μM.	19053768
CEM-SS	Function assay			Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50 = 0.127 μM.	14698189
COS7	Function assay			Antagonist activity at human CXCR4 V196A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.14 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells, IC50 = 0.1437 μM.	19451305
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 H281A mutant expressed in COS7 cells, Ki = 0.16 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 F172A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.17 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells, IC50 = 0.1753 μM.	19451305
COS7	Function assay			Antagonist activity at human CXCR4 H281A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.19 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells, IC50 = 0.1966 μM.	19451305
COS7	Function assay			Antagonist activity at human wild type CXCR4 expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.22 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells, IC50 = 0.2356 μM.	19451305
CEM	Function assay			Displacement of [125I]CXCL12 from CXCR4 in human CEM cells, IC50 = 0.245 μM.	19053768
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V99A mutant expressed in HEK293 cells, IC50 = 0.2585 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells, IC50 = 0.259 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 I284A mutant expressed in HEK293 cells, IC50 = 0.2658 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells, IC50 = 0.2891 μM.	19451305
COS7	Function assay			Antagonist activity at human CXCR4 H203A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM.	17599916
COS7	Function assay			Antagonist activity at transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 T287A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM.	17599916
HPBALL	Function assay		3 hrs	Displacement of 12G5-CXCL12 from CXCR4 in human HPBALL cells after 3 hrs by FACS analysis, IC50 = 0.29 μM.	29494843
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H113A mutant expressed in HEK293 cells, IC50 = 0.2964 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells, IC50 = 0.3002 μM.	19451305
CEM-SS	Antiviral assay			Antiviral activity against HIV1 LAI in human CEM-SS cells assessed as inhibition of viral replication, IC50 = 0.32 μM.	19356827
COS7	Function assay			Antagonist activity at human CXCR4 L120F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.33 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 Q200W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.4 μM.	17599916
MT4	Antiviral assay			Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral replication, IC50 = 0.41 μM.	19356827
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 E277A mutant expressed in HEK293 cells, IC50 = 0.4695 μM.	19451305
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200A mutant expressed in COS7 cells, Ki = 0.56 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells, IC90 = 0.5722 μM.	19451305
COS7	Function assay			Antagonist activity at human CXCR4 I259W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.63 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 Y255A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.66 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 H113A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.74 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells, IC90 = 0.7956 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells, IC90 = 0.8212 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells, IC90 = 0.8213 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells, IC90 = 0.8606 μM.	19451305
COS7	Function assay			Displacement of [125I]12G5 antibody from human wild type CXCR4 expressed in COS7 cells, Ki = 0.89 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 Q200A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.93 μM.	17599916
HEK293	Function assay			Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells, IC90 = 0.9302 μM.	19451305
HEK293	Function assay			Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells, IC90 = 0.9711 μM.	19451305
MDA-MB-231	Function assay		10 mins	Displacement of biotinylated TN14003 from CXCR4 CXCL12 binding domain in human MDA-MB-231 cells preincubated for 10 mins followed by biotinylated TN14003 addition measured after 30 mins using streptavidin-conjugated rhodamine by fluorescence microscopic a, EC = 1 μM.	27179215
MDA-MB-231	Function assay		10 mins	Inhibition of biotinylated TN14003 binding to CXCR4 in human MDA-MB-231 cells preincubated for 10 mins followed by TN14003 addition measured after 30 mins by rhodamine dye-based microscopic analysis, EC = 1 μM.	29529500
MDA-MB-231	Function assay		10 mins	Displacement of biotinylated-TN14003 from CXCR4 in human MDA-MB-231 cells assessed as reduction in fluorescence preincubated for 10 mins followed by biotinylated-TN14003 addition measured after 30 mins by streptavidin-rhodamine staining based microscopic , EC = 1 μM.	27914361
MDA-MB-231	Function assay		10 mins	Inhibition of biotinylated TN14003 binding to CXCR4 in human MDA-MB-231 cells assessed as reduction in fluorescence preincubated for 10 mins followed by biotinylated-TN14003 addition measured after 30 mins by streptavidin-rhodamine staining based immunofl, EC = 1 μM.	28521261
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 I284A mutant expressed in COS7 cells, Ki = 1.1 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 I284A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 1.2 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells, Ki = 1.5 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 H203A mutant expressed in COS7 cells, Ki = 1.8 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 D171N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 1.8 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 3 of human CXCR4 H113A mutant expressed in COS7 cells, Ki = 2 μM.	17599916
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D262N mutant, IC50 = 2.541 μM.	17599916
U87.CD4	Antiviral assay			Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D171ND262N mutant, IC50 = 2.694 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200W mutant expressed in COS7 cells, Ki = 2.7 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207F mutant expressed in COS7 cells, Ki = 2.7 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207W mutant expressed in COS7 cells, Ki = 3 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 T287A mutant expressed in COS7 cells, Ki = 3.1 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F174A mutant expressed in COS7 cells, Ki = 3.2 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D182A mutant expressed in COS7 cells, Ki = 3.2 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y256A mutant expressed in COS7 cells, Ki = 4 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 N176A mutant expressed in COS7 cells, Ki = 4.1 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 V196A mutant expressed in COS7 cells, Ki = 4.6 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259W mutant expressed in COS7 cells, Ki = 4.6 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F172A mutant expressed in COS7 cells, Ki = 4.7 μM.	17599916
COS7	Function assay			Antagonist activity at human CXCR4 D262N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 4.7 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 S263A mutant expressed in COS7 cells, Ki = 5.4 μM.	17599916
CCRF-CEM	Function assay		30 mins	Inhibition of anti-CXCR4 PE antibody clone 12G5 binding to CXCR4 in human CCRF-CEM cells preincubated for 30 mins followed by anti-CXCR4 PE antibody clone 12G5 addition measured after 30 mins by flow cytometric method, IC50 = 6.2 μM.	29125295
COS7	Function assay			Antagonist activity at human CXCR4 E288A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 6.4 μM.	17599916
MT4	Cytotoxicity assay			Cytotoxicity against human MT4 cells by MTT assay, CC50 = 6.5 μM.	19356827
COS7	Function assay			Antagonist activity at human CXCR4 A175F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 8.5 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y255A mutant expressed in COS7 cells, Ki = 9.7 μM.	17599916
MT-4	Function assay			Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells, EC50 = 10 μM.	9925728
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 D171N mutant expressed in COS7 cells, Ki = 13 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D187A mutant expressed in COS7 cells, Ki = 14 μM.	17599916
HL60	Function assay			Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells, IC50 = 15.2 μM.	19188071
COS7	Function assay			Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 A175F mutant expressed in COS7 cells, Ki = 36 μM.	17599916
COS7	Function assay			Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 D262N mutant expressed in COS7 cells, Ki = 46 μM.	17599916
COS, TZM-bl	Function assay			Inhibition of HIV1 NL4-3 envelope glycoprotein 120-mediated membrane fusion between virus-transfected african green monkey COS cells and human TZM-bl cells by luciferase-based cell-cell fusion assay in presence of IC9564	17954689
CXCR4+/CD4+/U87	Function assay			Inhibition of HIV1 92TH594 infected CXCR4+/CD4+/U87 cells to assess co-receptor tropism as luciferase activity	17116663
CXCR4+/CD4+/U87	Function assay			Inhibition of HIV1 HXB2 infected CXCR4+/CD4+/U87 cells to assess co-receptor tropism as luciferase activity	17116663
U87	Function assay	1000 nM		Antagonist activity at CXCR4 in human U87 cells assessed as inhibition of SDF1-induced modulation of cAMP production at 1000 nM by TR-FRET assay	17958344
CHOK1	Function assay			Induction of [125I]MCP1 dissociation from CCR2/CXCR4 expressed in CHOK1 cells by non-equilibrium binding assay	17715128
CHOK1	Function assay			Antagonist activity at CXCR4 expressed in CHOK1 cells assessed as inhibition of SDF1-alpha-induced signaling by aequorin-based assay	17715128
CHOK1	Function assay			Antagonist activity at CCR2/CXCR4 expressed in CHOK1 cells assessed as inhibition of SDF1-alpha-induced signaling by aequorin-based assay	17715128
CHOK1	Function assay			Induction of [125I]SDF1alpha dissociation from CXCR4 expressed in CHOK1 cells by non-equilibrium binding assay	17715128
U87.CD4	Function assay			Antagonist activity at human CXCR4 H281A mutant expressed in U87.CD4 cells assessed as inhibition of CXCL12-induced calcium mobilization	17599916
MT2	Antiviral assay	1 ug/mL	4 days	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral p24 antigen production at 1 ug/mL after 4 days by ELISA	21168336
MOLT4	Function assay	1000 nM		Inhibition of Mab 12G5 binding to CXCR4 expressed in human MOLT4 cells at 1000 nM by FACS analysis	19451305
TZM-bl	Antiviral assay	100 uM	24 hrs	Antiviral activity against HIV NL-Lai infected in human TZM-bl cells assessed as inhibition of viral infection at 100 uM treated before viral infection measured after 24 hrs by luciferase assay	21783371
Jurkat	Function assay	0.01 to 100 uM		Inhibition of CXCR4 in human Jurkat cells assessed as reduction in HIV-Nef-M1-induced mitochondrial membrane depolarization at 0.01 to 100 uM by JC1 dye based fluorescence depolarization assay	26191361
MDA-MB-231	Function assay	100 nM	24 hrs	Antagonist activity at CXCR4-mediated chemotaxis in human MDA-MB-231 cells assessed as inhibition of CXCL12-induced cell invasion at 100 nM after 24 hrs by crystal violet staining-based microscopic matrigel assay	29494843
TZM-bl	Antiviral assay		1 hr	Antiviral activity against HIV1 HXB2 pseudovirus infected in human TZM-bl cells assessed as inhibition of viral entry treated 1 hr post infection measured after 48 hrs by luciferase reporter gene assay	28266845
CXCR4+	Function assay	6 mg/kg	2 hrs	Induction hematopoietic stem cell mobilization in C57BL/6 mouse assessed as increase in CXCR4+ cells in blood at 6 mg/kg, sc measured after 2 hrs by APC-conjugated anti-CXCR4-staining based flow cytometry relative to vehicle control	29314840
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화학 정보, 보관 및 안정성

분자량	502.78	화학식	C₂₈H₅₄N₈	보관 (수령일로부터)	3년-20°C분말
CAS 번호	110078-46-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	JM 3100, SID791			Smiles	C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3

용해도

In vitro
배치:

Ethanol : 100 mg/mL

Water : 15 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 100 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : 100 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : 100 mg/mL

Water : 0.75 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Clear solution	5%absolute ethyl alcohol 1 40% PEG 300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.100mg/ml (2.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml absolute ethyl alcohol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% ethyl alcohol 1 95% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.100mg/ml (0.20mM)	Taking the 1 mL working solution as an example, add 50 μL of 2 mg/ml clear ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC₅₀/Ki	CXCL12 (Cell-free assay) 5.7 nM CXCR4 (Cell-free assay) 44 nM
시험관 내(In vitro)	Plerixafor (AMD3100)는 CXCR4에 대한 친화도보다 약간 더 나은 효능으로 CXCL12 매개 화학주성을 억제합니다. 또한 SDF-1/CXCL12 리간드 결합을 651 nM의 IC50으로 길항합니다. 이 화합물은 SDF-1 매개 GTP 결합, SDF-1 매개 칼슘 유출 및 SDF-1 자극 화학주성을 각각 27 nM, 572 nM 및 51 nM의 IC50으로 억제합니다. CXCR3, CCR1, CCR2b, CCR4, CCR5 또는 CCR7을 발현하는 세포에 대해 cognate 리간드로 자극했을 때 칼슘 유출을 억제하지 않으며, LTB4의 수용체 결합도 억제하지 않습니다. 그 자체로 CXCR4, CCR4 및 CCR7을 포함한 여러 GPCR을 발현하는 CCRF–CEM 세포에서 칼슘 유출을 유도하지 않습니다.
키나아제 분석	수용체 결합 분석
키나아제 분석	CXCR4에 대한 경쟁 결합 연구를 위해 Plerixafor (AMD3100)는 3시간 동안 4 °C에서 결합 버퍼(5 mM MgCl₂, 1 mM CaCl₂, 0.25% BSA, pH 7.4를 포함하는 PBS)에 5 × 10⁵ CCRF–CEM 세포와 100 pM ¹²⁵I-SDF-1α (2200 Ci/mmol)를 Milipore Durapore^TM 필터 플레이트에 넣어 배양합니다. 결합되지 않은 ¹²⁵I-SDF-1α는 차가운 50 mM HEPES, 0.5 M NaCl pH 7.4로 세척하여 제거합니다. BLT1에 대한 경쟁 결합 분석은 재조합 BLT1을 발현하는 CHO-S 세포의 막에서 수행됩니다. 막은 기계적 세포 용해 후 고속 원심분리로 준비하고, 50 mM HEPES, 5 mM MgCl₂ 버퍼에 재현탁한 후 급속 냉동합니다. 이 화합물은 실온에서 1시간 동안 막 준비물과 함께 50 mM Tris, pH 7.4, 10 mM MgCl₂, 10 mM CaCl₂, 4 nM LTB₄에 1 nM ³H-LTB₄ (195.0 Ci/mmol)를 혼합하고 8 μg 막을 포함하는 분석 혼합물에서 배양합니다. 결합되지 않은 ³H-LTB₄는 Millipore Type GF-C 필터 플레이트에서 여과하여 분리합니다.
생체 내(In vivo)	당뇨병 마우스에서 Plerixafor (AMD3100)를 한 번 국소 적용하면 사이토카인 생성을 증가시키고 골수 EPC를 동원하며 섬유아세포와 단핵구/대식세포의 활동을 향상시켜 혈관신생 및 혈관형성을 모두 증가시켜 상처 치유를 촉진합니다. 마우스 코호트에 5일 연속으로 PBS, IGF1, PDGF, SCF 또는 VEGF를 투여하고 5일째에 이 화합물을 투여합니다. IGF1과 이 화합물을 주사한 마우스에서 콜로니의 수와 크기가 PDGF, SCF 및 VEGF 처리군과 Plerixafor를 병용한 경우보다 가장 높았습니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/19641136/ [2] https://pubmed.ncbi.nlm.nih.gov/16815309/ [3] https://pubmed.ncbi.nlm.nih.gov/22048734/ [4] https://pubmed.ncbi.nlm.nih.gov/22342795/

적용 분야

방법	바이오마커	이미지	PMID
Immunofluorescence	β-arrestin2 CXCR4		31186083

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT05421416	Not yet recruiting	Stem Cell Transplant Complications	AHS Cancer Control Alberta	April 1 2024	Phase 2
NCT05343572	Recruiting	Asherman Syndrome\|Atrophic Endometrium\|Recurrent Implantation Failure	Hugh Taylor\|Yale University	November 1 2023	Early Phase 1
NCT05844527	Recruiting	Wound of Skin\|Abdominal Wound	MedRegen LLC	November 20 2023	Phase 2
NCT05411575	Withdrawn	COVID-19 Acute Respiratory Distress Syndrome\|COVID-19	4Living Biotech\|4P-Pharma	July 19 2022	Phase 2
NCT05445128	Terminated	Sickle Cell Disease	Ensoma\|bluebird bio	June 24 2022	Phase 2
NCT05835726	Recruiting	Multiple Myeloma\|Autologous Stem Cell Transplantation\|Leukapheresis	Fondazione Policlinico Universitario Agostino Gemelli IRCCS	January 1 2022	--

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자주 묻는 질문

질문 1:
How about the half-life of it (Cat S8030)?

답변:
Its biological half-life is 3-5 hours: https://en.wikipedia.org/wiki/Plerixafor.

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