Catalog No.S7772 Synonyms: GW120918
Molecular Weight(MW): 563.64
Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor.
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.
Purity & Quality Control
Choose Selective P-gp Inhibitors
|Description||Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor.|
Elacridar inhibits P-glycoprotein (P-gp) labeling by [3H]azidopine with a IC50 of 0.16 μM.  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. 
|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.  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.  In Mrp4(-/-) mice, elacridar fully inhibits P-gp mediated transport of topotecan, without siginificant effects on Bcrp1-mediated transport. |
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.
-  Tang SC, et al. Int J Cancer. 2014, 134(6), 1484-1494.
-  Hyafil F, et al. Cancer Res. 1993, 53(1), 4595-4602.
-  Sato H, et al. Eur J Pharmacol. 2015, 746, 258-266.
|In vitro||DMSO||41 mg/mL (72.74 mM)|
|In vivo||Add solvents individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*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).
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 )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.