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

Elacridar (GF120918) Chemical Structure

CAS: 143664-11-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) 810.81 现货
10mg 811.44 现货
50mg 2439.78 现货
200mg 6519.55 现货
1g 10401.3 现货
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常与Elacridar (GF120918)一起在实验中被使用的化合物

Imatinib


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。

Alves R, et al. Biomedicines. 2022 May 17;10(5):1158.

Sunitinib


Elacridar和Sunitinib抑制ABCG2功能并增强Sunitinib在786-O细胞中的细胞毒作用。

Sato H, et al. Eur J Pharmacol. 2015 Jan 5;746:258-66.

Ramucirumab (anti-VEGFR2)


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。

Schirizzi A, et al. Front Oncol. 2023 Feb 16;13:1129832.

TMZ(Temozolomide)


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。

Gooijer MCD, et al. Neoplasia. 2018 Jul;20(7):710-720.

Doxorubicin


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

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
P-gp [1] BCRP [1]
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]

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。

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]

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)

体外溶解度
批次:

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

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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