Home Transmembrane Transporters P-gp inhibitor Elacridar (GF120918) For research use only.

Elacridar (GF120918)

Synonyms: GW120918, GG918, GW0918

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

Elacridar (GF120918) Chemical Structure

Elacridar (GF120918) Chemical Structure

CAS: 143664-11-3

Selleck's Elacridar (GF120918) has been cited by 15 Publications

3 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.97%
99.97

Products often used together with Elacridar (GF120918)

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.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKVLB1 Cytotoxicity assay Cytotoxicity against human multidrug-resistant SKVLB1 cells in presence of adriamycin, IC50=0.02μM 11754602
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
Caco-2 Function assay Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells, EC50=2μM 17064079
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 human Pgp mediated [3H]vinblastine transport in human Caco-2 cells, EC50=2μM 17936633
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
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
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 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
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
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
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
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
Click to View More Cell Line Experimental Data

Biological Activity

Description 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.
Cell Research Cell lines ACHN, Caki-1, 786-O, and MCF-7 cells
Concentrations ~ 5 mM
Incubation Time 48 h
Method 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.
Experimental Result Images Methods Biomarkers Images 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]
Animal Research Animal Models Male wild-type, Abcb1a/1b-/-34, Abcg2 -/-32 and Abcb1a/1b;Abcg2
Dosages 100 mg/kg
Administration p.o.

Chemical lnformation & Solubility

Molecular Weight 563.64 Formula

C34H33N3O5
CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (177.41 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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