Elacridar (GF120918)

別名:GW120918, GG918, GW0918

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

Elacridar (GF120918)化学構造

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
JPY 22000 国内在庫あり
JPY 55500 国内在庫あり
JPY 119500 国内在庫あり
JPY 190500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(15)

カスタマーフィードバック3个实验数据

製品安全説明書

現在のバッチを見る: 純度: 99.97%
99.97

Elacridar (GF120918)と併用されることが多い化合物

Imatinib


Elacridar and Imatinib induce apoptosis, reduce cell proliferation rate, and arrest CML cells in the S phase.

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

Sunitinib


Elacridar and Sunitinib inhibit ABCG2 function and enhance the cytotoxic effects of sunitinib in 786-O cells.

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

Ramucirumab (anti-VEGFR2)


Elacridar and Ramucirumab can restore the inhibitory action of Paclitaxel on cell cycle progression in resistant GC cells.

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

TMZ(Temozolomide)


Elacridar and Temozolomide (TMZ) increase TMZ brain penetration and antitumor efficacy in wild-type mice.

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

Doxorubicin


Nanoparticles loaded with Doxorubicin and Elacridar are highly effective against HepG2 and HepG2-TS cells.

Chen D, et al. Int J Nanomedicine. 2018 Oct 25;13:6855-6870.

Elacridar (GF120918)関連製品

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
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
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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 inhibits P-glycoprotein (P-gp) labeling by [3H]azidopine with a IC50 of 0.16 μM. [2] In Caki-1 and ACHN cells, elacridar ( 2.5 μM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by elacridar. The combination of elacridar and sunitinib 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
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 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 3.0×103 cells per well are seeded in a 96-well plate. After 24 h incubation, an optimum concentration gradient of elacridar is added to each well. After culturing for 48 h, 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
Growth inhibition assay Cell viability 25862759
In Vivo
In Vivo Oral co-administration of elacridar (100 mg/kg, p.o.) and crizotinib increases the plasma and brain concentrations and brain-to-plasma ratios of crizotinib in wild-type mice, 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 elacridar 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, elacridar fully inhibits P-gp mediated transport of topotecan, 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.

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

In vitro
Batch:

DMSO : 100 mg/mL ( (177.41 mM); Warmed with 50℃ water bath; 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

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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)

mg/kg g μL

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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