Elacridar (GF120918)

Catalog No.S7772 Synonyms: GW120918

Elacridar (GF120918) Chemical Structure

Molecular Weight(MW): 563.64

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

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2 Customer Reviews

  • 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) is a potent P-gp (MDR-1) and BCRP inhibitor.
Targets
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 NIjwTGFEgXSxdH;4bYNqfHliYYPzZZk> M2LaSmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI12dHSrZIL1[{1z\XOrc4ThcpQhW0uYTFKxJINmdGy|IHnuJJBz\XOnbnPlJI9nKGGmcnnhcZlkcW5uIFnDOVA:OC5yMjFOwG0> MXuxNVc2PDZyMh?=
Kb-V1 cells NF;HUoJHfW6ldHnvckBie3OjeR?= NIXR[m8yOCCvaX7z Mkj6TY5pcWKrdHnvckBw\iCDQlPCNUBmgHC{ZYPz[YQhcW5iS3KtWlEh[2WubIOgZYZ1\XJiMUCgcYlveyCkeTDjZYxk\WmwLVHNJIF{e2G7LDDJR|UxRTBwMUmzJO69VQ>? Mn3GNlE2PzB{OEK=
MCF7/Topo cells M1[xTmZ2dmO2aX;uJIF{e2G7 NY\oWnVEUW6qaXLpeIlwdiCxZjDBRmNIOiCxdnXy[ZhxemW|c3XkJIlvKGi3bXHuJG1ETjdxVH;wc{Bk\WyuczDifUBndG:5IHP5eI9u\XS{aXOtZoF{\WRibXn0c5hidnS{b37lJIVn\my3eDDhd5NigSxiSVO1NF0xNjJ3IN88US=> M2TkblE6OTdyNUG5
MDCK2-MDR1 cells M4TaNGZ2dmO2aX;uJIF{e2G7 Mmq2OlAhdWmwcx?= MmDiTY5pcWKrdHnvckBw\iCqdX3hckBR\3Bib4\ldoV5eHKnc4Pl[EBqdiCqdX3hckBOTEONMj3NSHIyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gVlEzOyCnZn\seZgh[W[2ZYKgOlAhdWmwczygTWM2OD1yLkSg{txO NUPub481OjF2MUm2N|I>
HEK293 cells NYjST2ZJTnWwY4Tpc44h[XO|YYm= M3TNfGlvcGmkaYTpc44hd2ZiQVLDS|Ih\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bie3Onc4Pl[EBieyCvaYTvfIFvfHKxbnWtcYVlcWG2ZXSg[YZndHW6IHL5JIZtd3diY4n0c41mfHK7LDDJR|UxRTBwNEGg{txO NHrVOmQyPzNzN{G5Ny=>
MDCK cells Mmm5SpVv[3Srb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKEKFUmCg[ZhxemW|c3XkJIlvKE2GQ1ugZ4VtdHNiYomgdIhmd3Cqb4LibYRmKEFiYYPzZZktKEmFNUC9NE41OyEQvF2= NE\2fpYyQTl|Mkm2NC=>
SKVLB1 cells M2HuVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NEjzUoVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBufWy2aXTyeYcuemW|aYP0ZY51KFONVlzCNUBk\WyuczygTWM2OD1zLkSg{txO NELr[HkyOTd3NE[wNi=>
Caco-2 cells MUXGeY5kfGmxbjDhd5NigQ>? M1fyRWlvcGmkaYTpc44hd2ZiaIXtZY4hWC2pcDDt[YRq[XSnZDDbN2hefmmwYnzhd5RqdmVidILhcpNxd3K2IHHjeIl3cXS7IHnuJIh2dWGwIFPhZ48uOiClZXzsd{whTUN3ME2yJO69VQ>? NXThVmU4OTh{N{[xOFU>
SKOV3 cells NHHCSWpEgXSxdH;4bYNqfHliYYPzZZk> M3X5[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{NCCLQ{WwQVgvOSEQvF2= NXy5eohvOTF5NUS2NFI>

... Click to View More Cell Line Experimental Data

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]

Protocol

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Male wild-type, Abcb1a/1b-/-34, Abcg2 -/-32 and Abcb1a/1b;Abcg2
  • Formulation: Mixture of DMSO, Polysorbate 80, ethanol, and water (1.8:1.17:6.03:1, v/v/v/v)
  • Dosages: 100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 41 mg/mL (72.74 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
1mg/mL

* 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
Formula

C34H33N3O5

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID