Elacridar (GF120918)
别名: GW120918, GG918, GW0918 中文名称：依克立达
Elacridar (GF120918, GW120918, GG918, GW0918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。
Elacridar (GF120918) Chemical Structure
CAS: 143664-11-3
产品质控
批次：
纯度：
99.97%
99.97
常与Elacridar (GF120918)一起在实验中被使用的化合物
Elacridar和Imatinib诱导细胞凋亡，降低细胞增殖率，并将CML细胞阻滞在S期。
Elacridar和Sunitinib抑制ABCG2功能并增强Sunitinib在786-O细胞中的细胞毒作用。
Elacridar和Ramucirumab可以恢复Paclitaxel对耐药GC细胞细胞周期进展的抑制作用。
Elacridar和替莫唑胺(TMZ)可增加野生型小鼠中TMZ的脑渗透性和抗肿瘤功效。
载Doxorubicin和Elacridar的纳米粒对HepG2和HepG2-TS细胞有较好的杀伤作用。
Chen D, et al. Int J Nanomedicine. 2018 Oct 25;13:6855-6870.
Elacridar (GF120918)相关产品
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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 |
|---|---|---|---|---|---|
| primary mesothelioma stem cells | Function assay | 1 uM | 24 hrs | Inhibition of MDR1 in human primary mesothelioma stem cells assessed as increase in doxorubicin-induced reduction in cell viability at 1 uM after 24 hrs by by LDH release assay | 30584838 |
| primary glioblastoma stem cells | Function assay | 1 uM | 72 hrs | Inhibition of MDR1 in human primary glioblastoma stem cells assessed as increase in doxorubicin-induced reduction in cell viability at 1 uM after 72 hrs by ATPlite luminescence assay | 30584838 |
| primary mesothelioma stem cells | Function assay | 10 to 10000 nM | 3 hrs | Inhibition of MDR1 in human primary mesothelioma stem cells assessed as increase in intracellular doxorubicin accumulation at 10 to 10000 nM after 3 hrs by spectrofluorimetric analysis | 30584838 |
| primary glioblastoma stem cells | Function assay | 10 to 10000 nM | 3 hrs | Inhibition of MDR1 in human primary glioblastoma stem cells assessed as increase in intracellular doxorubicin accumulation at 10 to 10000 nM after 3 hrs by spectrofluorimetric analysis | 30584838 |
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| SKVLB1 | Cytotoxicity assay | Cytotoxicity against human multidrug-resistant SKVLB1 cells, IC50=1.4μM | 11754602 | ||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells, IC50=8.1μM | 11754602 | ||
| SKVLB1 | Cytotoxicity assay | Cytotoxicity against human multidrug-resistant SKVLB1 cells in presence of adriamycin, IC50=0.02μM | 11754602 | ||
| KBv1 | Function assay | Inhibition of ABCB1 overexpressed in human KBv1 cells by flow cytometric-based calcein-AM efflux assay, IC50=0.193μM | 19170519 | ||
| MCF7 MX | Function assay | Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining, IC50=0.4μM | 19932960 | ||
| MDCK | Function assay | Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50=0.43μM | 19932960 | ||
| MDCK2-MDR1 | Function assay | 60 mins | Inhibition of human Pgp overexpressed in human MDCK2-MDR1 cells assessed as inhibition of R123 efflux after 60 mins, IC50=0.4μM | 21419632 | |
| MCF7/Topo | Function assay | Inhibition of ABCG2 expressed in human MCF7/Topo cells by Hoechst microplate assay, IC50=0.127μM | 21570282 | ||
| Caco2 | Function assay | 3 uM | 30 mins | Inhibition of P-gp-mediated transport in human Caco2 cells at 3 uM after 30 mins | 22266779 |
| Kb-V1 | Function assay | 10 mins | Inhibition of ABCB1 expressed in Kb-V1 cells after 10 mins by calcein-AM assay, IC50=0.193μM | 21570282 | |
| Caco2 | Function assay | 3 uM | 30 mins | Inhibition of BCRP-mediated [3H]estrone-3-sulfate transport in human Caco2 cells at 3 uM after 30 mins | 22266779 |
| CCRF-CEM/VCR1000 | Function assay | Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis, IC50=0.07244μM | 22452412 | ||
| KBV1 | Function assay | 10 mins | Inhibition of ABCB1 in human KBV1 cells after 10 mins by Calcein-AM microplate assay, IC50=0.193μM | 24900683 | |
| MCF7/Topo | Function assay | 2 hrs | Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 microplate assay, IC50=0.127μM | 24900683 | |
| primary mesothelioma stem cells | Function assay | 1 uM | 72 hrs | Inhibition of MDR1 in human primary mesothelioma stem cells assessed as increase in doxorubicin-induced reduction in cell viability at 1 uM after 72 hrs by ATPlite luminescence assay | 30584838 |
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| primary glioblastoma stem cells | Function assay | 1 uM | 24 hrs | Inhibition of MDR1 in human primary glioblastoma stem cells assessed as increase in doxorubicin-induced reduction in cell viability at 1 uM after 24 hrs by by LDH release assay | 30584838 |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Elacridar (GF120918, GW120918, GG918, GW0918)是一种有效的P-gp (MDR-1) 和 BCRP 抑制剂。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Elacridar 抑制[3H]azidopine对P糖蛋白的标记，IC50值为0.16μM。[2] 在Caki-1和 ACHN细胞中，elacridar (2.5 μM)显著抑制细胞生长。Elacridar能够抑制P糖蛋白的活性。Elacridar 的联合使用显著降低ABC亚家族B分子2(ABCG2) 在786-O细胞中的表达。[3] |
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| 激酶实验 | P-gp 的光亲和性放射性标记 | |||
| 10 微升未标记的细胞膜悬液（蛋白量0.4 毫克/毫升)等分加入到96孔板中。然后每孔加5 微升GF120918。板在25℃下避光培养25 分钟。每孔加5 微升氚标记的azidopine(1.8 TBq/mmol)(0.6 μM in HCI 0.2 mM)。25℃下避光培养25 分钟后，用薄层色谱法设计的UV紫外灯直接与板接触，0℃下，254 nm 光照样品2 分钟。用十二烷基硫酸钠聚丙烯酰胺凝胶电泳的上样缓冲液溶解样品，但不加热。7.5%聚丙烯酰胺凝胶电泳分离后，凝胶经荧光放大处理，感光胶片曝光3天。用Camag薄层色谱扫描仪II密度计分析荧光显影。 | ||||
| 细胞实验 | 细胞系 | ACHN，Caki-1，786-O，和 MCF-7 细胞 | ||
| 浓度 | ~ 5 mM | |||
| 孵育时间 | 48小时 | |||
| 方法 | 以3000个细胞/孔的密度接种至96孔板中。培养24 小时后，将适宜浓度梯度的elacridar加至孔中。培养48 小时后，使用增殖试剂，MTT检测细胞活性。对照组细胞用载体（1% DMSO）处理。最终培育后，抽出培养基，沉淀的甲瓒晶体溶解在DMSO (100 微升/孔)中。每孔的吸光度在540 nm下测量，以650 nm为参比波长，在multiskan JX酶标仪上读取数据。细胞活性以对照组值的百分比计算。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Growth inhibition assay | Cell viability |
|
25862759 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在野生型小鼠中， elacridar (100 毫克/千克，腹腔注射) 口服联合给药，增加血浆和脑组织中的浓度，和大脑-血浆比值，与Abcb1a/1b; Abcg2-/-小鼠体内水平相当。[1] 在弗兰德白血病病毒染色的B模型小鼠中，elacridar静脉注射(2.5 毫克/千克)，腹腔注射(100毫克/千克)和口服 (100毫克/千克)后，大脑-血浆中的分配系数(Kp，大脑)分别为0.82， 0.43和 4.31。[4] 在Mrp4(-/-) 模型小鼠中，elacridar充分抑制P糖蛋白介导的转运，但是对Bcrp1介导的转运抑制效果有限。[5] |
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| 动物实验 | Animal Models | 雄性野生型，Abcb1a/1b-/-34，Abcg2 -/-32 和 Abcb1a/1b；Abcg2 |
| Dosages | 100 毫克/千克 | |
| Administration | 口服 | |
化学信息&溶解度
| 分子量 | 563.64 | 分子式 | C34H33N3O5 |
| CAS号 | 143664-11-3 | SDF | Download Elacridar (GF120918) SDF |
| Smiles | COC1=CC=CC2=C1NC3=C(C2=O)C=CC=C3C(=O)NC4=CC=C(C=C4)CCN5CCC6=CC(=C(C=C6C5)OC)OC | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (177.41 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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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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