1. Membrane Transporter/Ion Channel
  2. BCRP
    P-glycoprotein

Elacridar (Synonyms: GF120918; GW0918; GG918; GW120918)

Cat. No.: HY-50879 Purity: 98.47%
Data Sheet SDS Handling Instructions

Elacridar is a potent P-glycoprotein (Pgp) and BCRP inhibitor, used for cancer treatment.

For research use only. We do not sell to patients.
Elacridar Chemical Structure

Elacridar Chemical Structure

CAS No. : 143664-11-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
10 mg $60 In-stock
50 mg $210 In-stock
100 mg $310 In-stock
200 mg $500 In-stock
500 mg $1000 In-stock
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Other Forms of Elacridar:

    Elacridar purchased from MCE. Usage Cited in: J Drug Target. 2016;24(5):441-9.

    Cells are co-treated with 5 μM of free Raloxifene or an equivalent dose of SMA-raloxifene and either vehicle control (0.01% DMSO), Elacridar (1 μM), KO143 (5 μM), Valspodar (1 μM) or a combination of efflux inhibitors for 6 h.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Elacridar is a potent P-glycoprotein (Pgp) and BCRP inhibitor, used for cancer treatment.

    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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.7742 mL 8.8709 mL 17.7418 mL
    5 mM 0.3548 mL 1.7742 mL 3.5484 mL
    10 mM 0.1774 mL 0.8871 mL 1.7742 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [2]

    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°C 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°C in the dark, samples are simultaneously irradiated for 2 min at 254 nm at 0°C 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.
    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    Elacridar is dissolved in 0.1% DMSO.

    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[3].
    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Elacridar hydrochloride is dissolved in dimethyl sulfoxide (106 mg/mL).

    Mice are fasted for 3 hr before oral administration of either elacridar (100 mg/kg) or elacridar vehicle. Two hours later, crizotinib (5 mg/kg) is administered to mice orally. Blood and brains are isolated 4 hr after crizotinib oral administration, and processed as described above. The brain concentrations are corrected for the amount of drug in the brain vasculature. Elacridar hydrochloride is dissolved in dimethyl sulfoxide (106 mg/mL) in order to get 100 mg pure elacridar per 1 mL of dimethyl sulfoxide. The stock solution is further diluted with a mixture of Polysorbate 80, ethanol and water [20:13:67 (v/v/v)] to yield a concentration of 10 mg/mL pure elacridar.
    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    563.64

    Formula

    C₃₄H₃₃N₃O₅

    CAS No.

    143664-11-3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.47%

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    Product Name:
    Elacridar
    Cat. No.:
    HY-50879
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