Plerixafor (AMD3100)
别名: JM 3100, SID791 中文名称：普乐沙福
Plerixafor (AMD3100, JM 3100, SID791)是一种趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导的趋化性，无细胞试验中IC50分别为44 nM和5.7 nM。Plerixafor 可抑制human immunodeficiency virus (HIV)复制。
Plerixafor (AMD3100) Chemical Structure
CAS: 110078-46-1
产品质控
批次：
纯度：
99.89%
99.89
Plerixafor (AMD3100)相关产品
| 相关靶点 | CXCR1 CXCR2 CXCR4 CXCR3 | 点击展开 |
|---|---|---|
| 相关产品 | SB225002 WZ811 Reparixin (Repertaxin) LIT-927 Navarixin (SCH-527123) UNBS5162 LY2510924 AZD5069 AMD3465 hexahydrobromide AMG 487 SX-682 Danirixin (GSK1325756) MSX-122 | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I GPCR小分子化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| 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 | |
| MOLT4 | Function assay | 1000 nM | Inhibition of Mab 12G5 binding to CXCR4 expressed in human MOLT4 cells at 1000 nM by FACS analysis | 19451305 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| 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 NDK infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0019 μM. | 17599916 | ||
| U87.CD4 | Antiviral assay | Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0019 μM. | 17599916 | ||
| CHOK1 | Function assay | Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50 = 0.00081 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 CCR2/CXCR4 expressed in CHOK1 cells, IC50 = 0.00004 μM. | 17715128 | ||
| 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 | ||
| MT-4 | Function assay | Effective concentration against HIV-1(IIIB) replication in MT-4 cells, EC50 = 0.0042 μM. | 8568797 | ||
| MT-4 | Function assay | Effective concentration against HIV-2(ROD) replication in MT-4 cells, EC50 = 0.0059 μM. | 8568797 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
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生物活性
| 产品描述 | Plerixafor (AMD3100, JM 3100, SID791)是一种趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导的趋化性，无细胞试验中IC50分别为44 nM和5.7 nM。Plerixafor 可抑制human immunodeficiency virus (HIV)复制。 | ||||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Plerixafor抑制CXCL12介导的趋药性，效能稍微高于其对CXCR4的亲和力。[1] Plerixafor也会拮抗SDF-1/CXCL12配体结合，IC50 为651 nM。Plerixafor抑制SDF-1介导的GTP-结合，SDF-1介导的钙离子流和SDF-1刺激的趋药性，IC50 分别为27 nM，572 nM 和51 nM。用它们的同源配体刺激时，Plerixafor不抑制表达CXCR3，CCR1，CCR2b，CCR4，CCR5或者CCR7的细胞中钙离子流，Plerixafor也不会抑制LTB4的受体结合。Plerixafor自身不会在表达多重GPCRs ，包括CXCR4，CCR4和CCR7的CCRF–CEM细胞中诱导钙离子流。[2] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Immunofluorescence | CXCR4 β-arrestin2 |
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28521261 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在糖尿病小鼠体内，Plerixafor单剂量局部给药促进伤口愈合，通过增加细胞因子产生，动员骨髓EPCs，并增强成纤维细胞和单核细胞/巨噬细胞，从而增加血管新生和血管生成发挥作用。[3] 同类小鼠以PBS，IGF1，PDGF，SCF，或VEGF连续给药5天，在第5天给药Plerixafor。与PDGF，SCF和VEGF结合Plerixafor的试验组相比，IGF1加Plerixafor的注射小鼠中，菌落的数量和大小最高。[4] |
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|---|---|---|
| 动物实验 | Animal Models | 节段性骨缺损的12周大C57BL/6小鼠 |
| Dosages | 5 mg/kg | |
| Administration | i.p. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 | -- |
化学信息&溶解度
| 分子量 | 502.78 | 分子式 | C28H54N8 |
| CAS号 | 110078-46-1 | SDF | Download Plerixafor (AMD3100) SDF |
| Smiles | C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
Ethanol : 100 mg/mL (198.89 mM) DMSO : Insoluble ( ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
How about the half-life of the product (Cat S8030)?
回答：
The biological half-life for this drug is 3-5 hours: https://en.wikipedia.org/wiki/Plerixafor.
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