Elacridar (GF120918)

別名：GW120918, GG918, GW0918

製品コード：S7772 純度：99.97%

Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.

CAS No. 143664-11-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
200mg	JPY 119500	国内在庫あり
1g	JPY 190500	国内在庫あり

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（28）

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製品安全説明書

現在のバッチを見る：純度： 99.97%

99.97

Elacridar (GF120918)関連製品

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シグナル伝達経路

P-gpシグナル伝達経路

P-gp阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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生物活性

製品説明

Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.

Targets

P-gp ^[1]

BCRP ^[1]

In Vitro
In vitro	Elacridar (GF120918) inhibits P-glycoprotein (P-gp) labeling by [³H]azidopine with a IC50 of 0.16 μM. ^[2] In Caki-1 and ACHN cells, it ( 2.5 μM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by this compound. Its combination lead to a significant reduction in ABC Sub-family B Member 2 (ABCG2) expression in 786-O cells. ^[3]
Kinase Assay	Photoaffinity radiolabeling of P-gp
Kinase Assay	10 μL of unlabeled cell membrane suspension (at 0.4 mg of protein/mL) are aliquoted into each well in 96-well plates. 5 μL of Elacridar (GF120918) are then added to each well. The plate is incubated 25 min at 25℃ in the dark. 5 μL of tritiated azidopine (1.8 TBq/mmol) (0.6 μM in HCI 0.2 mM) are added to each well. After 25 min of incubation at 25℃ in the dark, samples are simultaneously irradiated for 2 min at 254 nm at 0℃ with a thin layer chromatography-designed UV lamp directly in contact with the plate. Samples are solubilized in sodium dodecyl sulfate-polyacrylamide gel electrophoresis sample buffer but not heated. After separation on a 7.5% polyacrylamide gel, the gel is treated for fluorography with Amplify and exposed during 3 days onto a photosensitive film. The fluorography is analysed using a Camag thin layer chromatography Scanner II densitometer.
細胞実験	細胞株	ACHN, Caki-1, 786-O, and MCF-7 cells
	濃度	~ 5 mM
	反応時間	48 h
	実験の流れ	After seeding 3.0×10³ cells per well in a 96-well plate and incubating for 24 h, an optimum concentration gradient of Elacridar (GF120918) is added to each well. Following a 48 h culture period, cell viability is assessed using the proliferation reagent, MTT. Control cells are treated with the vehicle only, 0.1% DMSO. After this final incubation, the medium is aspirated and precipitated formazan crystals are dissolved in DMSO (100 µL/well). The absorbance of each well is measured at 540 nm, and a reference wavelength of 650 nm is read with a multiskan JX microplate reader. Cell viability is calculated as percentage of the control value.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Growth inhibition assay	Cell viability		25862759

In Vivo
In Vivo	Elacridar (GF120918) increases plasma and brain concentrations and brain-to-plasma ratios in wild-type mice when co-administered orally (100 mg/kg, p.o.), equaling the levels in Abcb1a/1b; Abcg2^-/- mice. ^[1] In friend leukemia virus stain B mice, the brain-to-plasm partition coefficient (Kp, brain) of this compound is 0.82, 0.43, and 4.31 after intravenous (2.5 mg/kg), intraperitoneal (100 mg/kg), and oral (100 mg/kg) treatment, respectively. ^[4] In Mrp4(-/-) mice, it fully inhibits P-gp mediated transport, without siginificant effects on Bcrp1-mediated transport. ^[5]
動物実験	動物モデル	Male wild-type, Abcb1a/1b^-/-34, Abcg2 ^-/-32 and Abcb1a/1b;Abcg2
	投与量	100 mg/kg
	投与経路	p.o.

参考
https://pubmed.ncbi.nlm.nih.gov/24037730/ https://pubmed.ncbi.nlm.nih.gov/8402633/ https://pubmed.ncbi.nlm.nih.gov/25455500/ https://pubmed.ncbi.nlm.nih.gov/22611067/ https://pubmed.ncbi.nlm.nih.gov/17975156/ + 展開

参考

https://pubmed.ncbi.nlm.nih.gov/24037730/
https://pubmed.ncbi.nlm.nih.gov/8402633/
https://pubmed.ncbi.nlm.nih.gov/25455500/

https://pubmed.ncbi.nlm.nih.gov/22611067/
https://pubmed.ncbi.nlm.nih.gov/17975156/

+ 展開

化学情報

分子量	563.64	化学式	C₃₄H₃₃N₃O₅
CAS No.	143664-11-3	SDF	Download Elacridar (GF120918) SDFをダウンロードする
Smiles	COC1=CC=CC2=C1NC3=C(C2=O)C=CC=C3C(=O)NC4=CC=C(C=C4)CCN5CCC6=CC(=C(C=C6C5)OC)OC
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (177.41 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.				投与溶液組成計算機
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 30%PEG300 2 5%Tween80 3 61%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.000mg/ml (1.77mM)	Taking the 1 mL working solution as an example, add 40 μL 25 mg/ml clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 610 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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