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    Elacridar (GF120918)
    Elacridar (GF120918)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1296
    CAS #: 143664-11-3 Purity ≥98%

    Description: Elacridar (formerly GW-120918; GF-120918; GG-918; GW-0918; GF120918; GF120918; GW0918; GG918) is a 3rd generationl and potent P-glycoprotein (P-gp or MDR-1) and BCRP inhibitor that has the potential to overcome P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs such as doxorubicin. Elacridar has been used both in vitro and in vivo as a tool inhibitor of P-gp to investigate the role of transporters in the disposition of various test molecules. In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma.

    References: Int J Cancer. 2014 Mar 15;134(6):1484-94; Drug Metab Dispos. 2012 Aug;40(8):1612-9; Clin Cancer Res. 2007 Nov 1;13(21):6440-9.

    Related CAS#:143851-98-3 (HCl); 143664-11-3 (Elacridar)

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    Molecular Weight (MW)563.64
    FormulaC34H33N3O5 
    CAS No.143664-11-3 (free); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 41 mg/mL (72.7 mM)
    Water:<1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 1 mg/mL
    SynonymsGW120918; GF-120918; GW 120918; GG-918; GW-0918; GF 120918; GW120918; GW0918; GF120918; GW 0918; GG918; GG 918;


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    In Vitro

    In vitro activity: 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. 


    Kinase Assay: 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 Assay: 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.

    In VivoOral 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.
    Animal modelMale wild-type, Abcb1a/1b-/-34, Abcg2 -/-32 and Abcb1a/1b;Abcg2
    Formulation & DosageDissolved in mixture of DMSO, Polysorbate 80, ethanol, and water (1.8:1.17:6.03:1, v/v/v/v); 100 mg/kg ; p.o.
    References

    Int J Cancer. 2014 Mar 15;134(6):1484-94; Drug Metab Dispos. 2012 Aug;40(8):1612-9; Clin Cancer Res. 2007 Nov 1;13(21):6440-9.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Elacridar (GF120918)A, brain concentrations of topotecan in WT, Mdr1a/b(−/−) (P-gp knockout), Bcrp1(−/−) (Bcrp1 knockout), and Mdr1a/b(−/−)Bcrp1(−/−) (compound P-gp and Bcrp1 knockout) mice at t = 1, 4, 8, 12, and 24 h after dosing. B, brain versus plasma concentration ratios in mice receiving topotecan (single agent; left) and in combination with elacridar (right). Clin Cancer Res. 2007 Nov 1;13(21):6440-9.
     

    Elacridar (GF120918)

    A, plasma concentration-time profile of topotecan in WT, Mdr1a/b(−/−), Bcrp1(−/−), and Mdr1a/b(−/−)Bcrp1(−/−) mice receiving topotecan as single agent. B, plasma concentration-time profile of topotecan in WT, Mdr1a/b(−/−), Bcrp1(−/−), and Mdr1a/b(−/−)Bcrp1(−/−) mice receiving topotecan in combination with elacridar.  Clin Cancer Res. 2007 Nov 1;13(21):6440-9.
     

    Elacridar (GF120918)

    A, elacridar concentrations in plasma and brain after a single oral dose of 100 mg/kg in FVB wild-type mice.  B, brain-to-plasma concentration ratios for elacridar after a single oral dose of 100 mg/kg in FVB wild-type mice. Drug Metab Dispos. 2012 Aug;40(8):1612-9. 


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