Elacridar (GF120918)

别名: GW120918, GG918, GW0918 中文名称：依克立达

目录号：S7772 Purity: 99.97%

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

规格	价格	库存
10mM (1mL in DMSO)	RMB 810.81	现货
10mg	RMB 811.44	现货
50mg	RMB 2439.78	现货
200mg	RMB 6519.55	现货
1g	RMB 10401.3	现货
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客户使用Selleck的Elacridar (GF120918)发表文献15篇

客户使用该产品的3个实验数据

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

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

相关化合物库	FDA药物库天然产物库离子通道配体库外泌体分泌相关化合物库钙通道阻滞剂库	点击展开

P-gp抑制剂选择性比较

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
Caco2	Function assay	3 uM	30 mins	Inhibition of P-gp-mediated [3H]-digoxin transport in human Caco2 cells at 3 uM after 30 mins	22266779
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
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
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	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	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
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
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
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
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
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
KBV1	Function assay		10 mins	Inhibition of ABCB1 in human KBV1 cells after 10 mins by Calcein-AM microplate assay, IC50=0.193μM	24900683
Caco-2	Function assay			Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells, EC50=2μM	17936633
HEK293	Function assay			Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry, IC50=0.41μM	17317193
Caco-2	Function assay			Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells, EC50=2μM	17064079
SKOV3	Cytotoxicity assay			Cytotoxicity against human SKOV3 cells, IC50=8.1μM	11754602
SKVLB1	Cytotoxicity assay			Cytotoxicity against human multidrug-resistant SKVLB1 cells, IC50=1.4μM	11754602
SKVLB1	Cytotoxicity assay			Cytotoxicity against human multidrug-resistant SKVLB1 cells in presence of adriamycin, IC50=0.02μM	11754602
Caco-2	Function assay			Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells, EC50=2μM	18257545
Caco-2	Function assay			Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells, EC50=2μM	18276145
Caco-2	Function assay			Inhibition of ABCB1-mediated [3H]vinblastine transportation in human Caco-2 cells, IC50=2μM	19053888
KBv1	Function assay			Inhibition of ABCB1 overexpressed in human KBv1 cells by flow cytometric-based calcein-AM efflux assay, IC50=0.193μM	19170519
MCF7/Topo	Function assay			Inhibition of ABCG2 overexpressed in human MCF7/Topo cells by flow cytometric-based mitoxantrone efflux assay, IC50=0.25μM	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
MCF7/Topo	Function assay			Inhibition of ABCG2 expressed in human MCF7/Topo cells by Hoechst microplate assay, IC50=0.127μM	21570282
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
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
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
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
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 和sunitinib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
激酶实验	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
实验图片	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) 和crizotinib口服联合给药，增加血浆和脑组织中crizotinib的浓度，和crizotinib的大脑-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topotecan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

参考文献
[1] Tang SC, et al. Int J Cancer. 2014, 134(6), 1484-1494. [2] Hyafil F, et al. Cancer Res. 1993, 53(1), 4595-4602. [3] Sato H, et al. Eur J Pharmacol. 2015, 746, 258-266. [4] Sane R, et al. Drug Metab Dispos. 2012, 40(8), 1612-1619. [5] de Vries NA, et al. Clin Cancer Res. 2007, 13(21), 6440-6449. + 展开

参考文献

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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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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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