Applications
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In H3255, HCC827 and H1975 cells, EGF816 significantly lowered pEGFR levels with EC50 values of 5, 1 and 3 nM, respectively. In addition, EGF816 inhibited proliferation of H3255, HCC827 and H1975 cells with EC50 values of 9, 11 and 25 nM, respectively.
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Applications
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In H1975 mouse xenograft models, EGF816 (10 mg/kg) significantly inhibited tumor growth with a T/C value of 29%. At higher doses of 30 and 100 mg/kg, EGF816 inhibited tumor growth with T/C values reaching ~ 60% and ~ 80%, respectively.
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References:
[1]. Jia Y, Juarez J, Li J, Manuia M, Niederst MJ, Tompkins C, Timple N, Vaillancourt MT, Pferdekamper AC, Lockerman EL, Li C, Anderson J, Costa C, Liao D, Murphy E, DiDonato M, Bursulaya B, Lelais G, Barretina J, McNeill M, Epple R, Marsilje TH, Pathan N, Engelman JA, Michellys PY, McNamara P, Harris J, Bender S, Kasibhatla S. EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor. Cancer Res. 2016 Mar 15;76(6):1591-602.
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