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    Pelitinib (EKB-569; WAY-EKB 569)
    Pelitinib (EKB-569; WAY-EKB 569)

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0553
    CAS #: 257933-82-7Purity ≥98%

    Description: Pelitinib (formerly EKB569; WAY-EKB569; WAY-172569), a 3-cyanoquinoline analog, is an irreversible/covalent EGFR inhibitor with potential antineoplastic activity. It inhibits epidermal growth factor receptor-EGFR with an IC50 of 38.5 nM, more selective for inhibiting EGFR  over c-Met, Src, erbB-2, Raf, Cdk4. 

    References: Nat Med. 2000 Sep;6(9):1024-8; Mol Cancer Ther. 2004 Jan;3(1):21-7; J Clin Invest. 2006 Feb;116(2):309-21.

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    Molecular Weight (MW)467.92
    CAS No.257933-82-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 13 mg/mL (27.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL 
    SynonymsPelitinib; EKB569; WAY-172569; EKB-569; EKB 569; WAY 172569; WAY172569 

    Chemical Name: (E)-N-(4-((3-chloro-4-fluorophenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide


    InChi Code: InChI=1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+

    SMILES Code: O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(F)C(Cl)=C3)C2=C1)/C=C/CN(C)C

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    In Vitro

    In vitro activity: Pelitinib displays much higher inhibitory activity against EGFR, compared with the closely related c-erbB-2, as well as other kinases such as Src, Cdk4, c-Met, Raf, and MEK/ERK, with IC50 ranging from 282 nM for Src to >20 μM for Cdk4. Consistently, Pelitinib treatment significantly inhibits the autophosphorylation of EGFR but not c-Met in A431 cells. Pelitinib potently inhibits the proliferation of normal human keratinocytes (NHEK), as well as A431 and MDA-468 tumor cells with IC50 of 61 nM, 125 nM, and 260 nM, respectively, while displaying little activity against MCF-7 cells with IC50 of 3.6 μM. Pelitinib inhibits EGF-induced phosphorylation of EGFR in A431 and NHEK cells with IC50 of 20-80 nM, as well as the phosphorylation of STAT3 with IC50 of 30-70 nM. Pelitinib at 75-500 nM also specifically inhibits the activation of AKT and ERK1/2, without affecting NF-κB pathway. In NHEK cells, Pelitinib also potently inhibits TGF-α mediated EGFR activation with IC50 of 56 nM, as well as activation of STAT3 and ERK1/2 with IC50 of 60 nM and 62 nM, respectively.

    Kinase Assay: For experiments using cells in culture, A431 cells are treated with various concentrations of Pelitinib for 2.75 hours before co-incubation with 100 ng/mL EGF for 0.25 hour. Cells are washed twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer (10 mM Tris, pH 7.5, 5 mM ethylenediamine tetra-acetic acid (EDTA), 150 mM NaCl, 1% Triton X-100, 1% Sodium deoxycholate, 0.1 % SDS, 1 mM PMSF, 10 mg/mL pepstatin A, 10 mg/mL leupeptin, 20 KIU/mL aprotinin, 2 mM sodium orthovanadate, and 100 mM sodium fluoride) for 20 minutes on ice, before immunoprecipitation and SDS-PAGE-immunoblotting. For immunoprecipitation, cultured cells are placed in cold lysis buffer and immediately homogenized on ice with a polytron with several pulses. The homogenate is first centrifuged at 2500 rpm (20 minutes, 4 °C) and then again at 14,000 rpm in a microcentrifuge (10 minutes, 4 °C). Supernatants (1000 μg protein) are incubated for 2 hours at 4 °C with 15 mL of EGFR polyclonal antibody. After 2 hours, 50 μL of protein G plus/protein A agarose beads is added and incubated with constant rotation for 2 hours at 4 °C. After washing with lysis buffer, beads are boiled for 2 minutes in Laemmli sample buffer. Proteins are then resolved by SDS-PAGE, transferred to immobilon membrane and probed overnight with an anti-phosphotyrosine antibody conjugated with horseradish peroxidase (HRP). Membranes are developed using the ECL reagent. Total EGFR protein is determined by stripping membranes and re-probing with receptor-specific antibodies. Quantitation of bands is done by densitometry, using ImageQuant software with a Molecular Dynamics laser transmittance scanner.

    Cell Assay: Cells (NHEK, A431, MCF-7, and MDA-468) are seeded in 96-well dishes, and after 2 hours, Pelitinib is added and incubated for 5 days. After incubation, the medium is removed from each well and fresh medium (150 μL) + 1 mg/mL MTT solution (50 μL) is added. After incubation for 2 hours at 37 °C, the medium is replaced with 150 μL DMSO, and absorbance at 540 nm in each well is determined. The IC50 is calculated by linear regression of the data.

    In VivoA single oral dose of 10 mg/kg Pelitinib potently inhibits the EGFR phosphorylation in A431 xenografts with over-expressed EGFR, by 90% within 1 hour, and by >50% after 24 hours. Administration of Pelitinib at 20 mg/kg/day inhibits tumorigenesis in APCMin/+ mice by 87%, equivalent to the effect of used with 2 times doses of EKI-785 (40 mg/kg/day), consistent with greater in vivo potency. Pelitinib selectively inhibits EGFR signaling in airway epithelial cells in vivo. In the mouse model of airway epithelial remodeling that is inducible by viral infection and features a delayed but permanent switch to goblet cell metaplasia, Pelitinib treatment at 20 mg/kg/day corrects all 3 aspects of epithelial remodeling, by completely blocking the increase of ciliated cells and decrease of Clara cells, and significantly inhibiting the metaplasia of goblet cells.
    Animal modelAthymic nu/nu female mice bearing subcutaneous A431 tumors, or APCMin/+ male mice, a murine model of human familial adenomatous polyposis (FAP)
    Formulation & DosageDissolved in pH 2.0 water;  10, or 20 mg/kg/day; Oral gavage

    Nat Med. 2000 Sep;6(9):1024-8; Mol Cancer Ther. 2004 Jan;3(1):21-7; J Clin Invest. 2006 Feb;116(2):309-21.

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

    Pelitinib (EKB-569)

    Cell surface expression and functional analysis of ABCG2 and ABCB1 in A549 cells with or without hyperthermia (42.5°C) treatment.  2015 Aug;172(16):4089-106.

    Pelitinib (EKB-569)

    Inhibition of ABCB1-, ABCC1- or ABCG2-mediated efflux of fluorescent probe substrate by pelitinib in drug-resistant cells overexpressing the transporters (left panel) or HEK293 cells stably transfected with the three transporters (right panel).  2015 Aug;172(16):4089-106.

    Pelitinib (EKB-569)

    Inhibition kinetics of ABCB1- and ABCG2-mediated topotecan efflux by pelitinib. 2015 Aug;172(16):4089-106.

    Pelitinib (EKB-569)Effect of pelitinib on the ATPase activity of ABCB1 (top panel) and ABCG2 (bottom panel).  2015 Aug;172(16):4089-106.

    Pelitinib (EKB-569)

    mRNA and cell surface expression of ABCB1 and ABCG2 in A549 after treatment with pelitinib.  2015 Aug;172(16):4089-106.

    Pelitinib (EKB-569)

    elitinib sensitized A549 cells to apoptosis specifically after exposure to hyperthermia.  2015 Aug;172(16):4089-106.


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