Elacridar (GF120918)
Catalog No.S7772 Synonyms: GW120918
Molecular Weight(MW): 563.64
Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor.
Cited by 1 Publication
1 Customer Review
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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.
Purity & Quality Control
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Biological Activity
| Description | Elacridar (GF120918) is a potent P-gp (MDR-1) and BCRP inhibitor. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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. |
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| Cell Research:[3] |
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| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 41 mg/mL (72.74 mM) |
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| 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 |
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| Formula | C34H33N3O5 |
| CAS No. | 143664-11-3 |
| Storage | powder |
| Synonyms | GW120918 |
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