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Elacridar (GF120918)

For research use only.

Catalog No.S7772 Synonyms: GW120918

7 publications

Elacridar (GF120918) Chemical Structure

CAS No. 143664-11-3

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

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Selleck's Elacridar (GF120918) has been cited by 7 publications

3 Customer Reviews

  • Impact of 10 μM elacridar on the intracellular accumulation of 10 μM nintedanib in DMS114 and DMS114/NIN cells was analyzed by confocal fluorescence microscopy after 1 h drug exposure. The scale bar indicates 10 μm.

    J Exp Clin Cancer Res, 2017, 36(1):122. Elacridar (GF120918) purchased from Selleck.

    Effect of drugs on the photo-crosslinking of cysless WT and triple A (Y307A/Q725A/Y953A) mutant P-gp with IAAP. Crude membranes expressing cysless WT or mutant P-gp (60-80 μg protein) were treated with the indicated concentrations of drug in 100 μL buffer containing 50 mM MES-Tris pH 6.8 for 10 min at 37 °C. Samples were then photo-crosslinked with 4–6 nM IAAP at 4 °C as described in Section 2. IAAP-labeling of the cysless WT and Triple A mutant P-gp with no addition of drug was taken as 100% labeling. Both panels show a representative autoradiogram (at the top) and the quantification of the IAAP-labeling (at the bottom). Lane 1, control (DMSO solvent); 2, 1 μM zosuquidar; 3, 1 μM elacridar; and 4, 1 μM tariquidar. Data represent the mean ± the standard deviations for n = 3. Left panel, cysless WT; right panel, Triple A (Y307A/Q725A/Y953A) mutant.

    Biochem Pharmacol, 2016, 101:40-53.. Elacridar (GF120918) purchased from Selleck.

  • Y953A mutant P-gp displays significantly decreased reversal of transport function by zosuquidar, tariquidar and elacridar. The upper panels (A-C) show the histograms for the transport of NBDCsA by the cysless WT and Y953A mutant P-gps. The histograms also show the effect of 50 nM zosuquidar (A), 50 nM tariquidar (B) or 50 nM elacridar (C) on reversal of NBDCsA transport by Y953A mutant P-gp, and by cysless WT P-gp (traces with maximum fluorescence intensity). The lower panels (D–F) show the effect of zosuquidar, tariquidar and elacridar at indicated concentrations on reversal of NBDCsA transport by cysless WT and Y953A mutant P-gp. The transport of NBDCsA in the absence of any inhibitor was taken as 100% for both cysless WT and Y953A mutant, respectively, and the percent of transport in the presence of the different inhibitors was calculated with respect to it. Data points are plotted as the mean + SD (n=3). The values of IC50 (compound concentration that produces 50% inhibition of NBDCsA transport in HeLA cells expressing cysless WT or Y953A mutant P-gp) are given in the figure. The IC50 value of zosuquidar could not be calculated, as a maximum 20% inhibition was observed at the highest concentration. The data was plotted and IC50 values calculated using GraphPad Prism 6.0.

    Biochem Pharmacol, 2016, 101:40-53. Elacridar (GF120918) purchased from Selleck.

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Biological Activity

Description Elacridar (GF120918, GW120918) is a potent P-gp (MDR-1) and BCRP inhibitor.
P-gp [1] BCRP [1]
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKVLB1 cells M2rndmN6fG:2b4jpZ4l1gSCjc4PhfS=> MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDteYx1cWS{dXetdoV{cXO2YX70JHNMXkyEMTDj[YxteyCrbjDwdoV{\W6lZTDv[kBi\HKrYX35Z4lvNCCLQ{WwQVAvODJizszN M{G1NVEyPzV2NkCy
Kb-V1 cells NGrk[5lHfW6ldHnvckBie3OjeR?= MlTHNVAhdWmwcx?= NXXFU3VuUW6qaXLpeIlwdiCxZjDBRmNDOSCneIDy[ZN{\WRiaX6gT4IuXjFiY3XscJMh[W[2ZYKgNVAhdWmwczDifUBk[WylZXnuMWFOKGG|c3H5MEBKSzVyPUCuNVk{KM7:TR?= NIn0eZUzOTV5MEK4Ni=>
MCF7/Topo cells M{T2SmZ2dmO2aX;uJIF{e2G7 NXPVNm9DUW6qaXLpeIlwdiCxZjDBRmNIOiCxdnXy[ZhxemW|c3XkJIlvKGi3bXHuJG1ETjdxVH;wc{Bk\WyuczDifUBndG:5IHP5eI9u\XS{aXOtZoF{\WRibXn0c5hidnS{b37lJIVn\my3eDDhd5NigSxiSVO1NF0xNjJ3IN88US=> MkLLNVkyPzB3MUm=
MDCK2-MDR1 cells MkDtSpVv[3Srb36gZZN{[Xl? NYXUeFYyPjBibXnudy=> Mn\MTY5pcWKrdHnvckBw\iCqdX3hckBR\3Bib4\ldoV5eHKnc4Pl[EBqdiCqdX3hckBOTEONMj3NSHIyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gVlEzOyCnZn\seZgh[W[2ZYKgOlAhdWmwczygTWM2OD1yLkSg{txO NG\PSWIzOTRzOU[zNi=>
HEK293 cells NXTCc3loTnWwY4Tpc44h[XO|YYm= NFrFNHlKdmirYnn0bY9vKG:oIFHCR2czKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNibXn0c5hidnS{b37lMY1m\GmjdHXkJIVn\my3eDDifUBndG:5IHP5eI9u\XS{eTygTWM2OD1yLkSxJO69VQ>? MX6xO|MyPzF7Mx?=
SKVLB1 cells M{XrNmN6fG:2b4jpZ4l1gSCjc4PhfS=> Moe0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcZVtfGmmcoXnMZJme2m|dHHueEBUU1[OQkGgZ4VtdHNuIFnDOVA:OS52IN88US=> Mn;FNVE4PTR4MEK=
Caco-2 cells NWXBT2oyTnWwY4Tpc44h[XO|YYm= NVjVNFJoUW6qaXLpeIlwdiCxZjDoeY1idiCSLXfwJI1m\GmjdHXkJHs{UF24aX7icIF{fGmwZTD0doFve3CxcoSgZYN1cX[rdImgbY4hcHWvYX6gR4Fkdy1{IHPlcIx{NCCHQ{WwQVIh|ryP MorTNVgzPzZzNEW=
SKOV3 cells M4HvVmN6fG:2b4jpZ4l1gSCjc4PhfS=> NFG1coZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyxiSVO1NF05NjFizszN NHfqV24yOTd3NE[wNi=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Growth inhibition assay
Cell viability ; 

PubMed: 25862759     

IC50 curve of GL261 glioma cells with elacridar (ELD). IC50=5.8 μM

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]


Kinase Assay:[2]
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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:[3]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Male wild-type, Abcb1a/1b-/-34, Abcg2 -/-32 and Abcb1a/1b;Abcg2
  • Dosages: 100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 8 mg/mL warmed (14.19 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 563.64


CAS No. 143664-11-3
Storage powder
in solvent
Synonyms GW120918

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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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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P-gp Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID