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3 protocols using pelitinib

1

Comparative Analysis of Tyrosine Kinase Inhibitors

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Total 11 TKIs were tested in this study. DMSO was used as a solvent for the TKIs and also as the negative vehicle control. Pyrimethamine 5 μM was used for positive control. Afatinib (BIBW2992), AG1478, dacomitinib (PF299), erlotinib (OSI-420), gefitinib (ZD1839), lapatinib, neratinib, AZD9291 (osimertinib), pelitinib, and nintedanib (BIBF 1120) were purchased from Selleck Chemicals (Houston, Texas, USA). Dimethyl sulfoxide (DMSO), pyrimethamine, and sunitinib malate (SU 11248) were purchased from Sigma Aldrich (St. Louis, Missouri, USA).
Bovine serum albumin was purchased from Bovogen Biologicals (Melbourne, Australia). Antibodies against β-actin were purchased from Cell Signaling Technology (Beverly, Massachusetts, USA). FITC-conjugated anti-mouse IgG antibody, TRTIC-conjugated anti-rabbit IgG antibody, and horseradish peroxidase-conjugated anti-rabbit or anti-mouse antibodies were purchased from Sigma Aldrich. Mouse Tg563 monoclonal antibody was cloned in our laboratory. PDCD4 (D29C6) XP® anti-rabbit monoclonal antibody was purchased from Cell Signaling.
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2

Small Molecule Inhibitor Sourcing and Preparation

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All small molecule inhibitors were purchased from Selleck Chemicals: BYL719 (S2814), GDC0941 (S1065), pelitinib (S1392), everolimus (S1120), AZD8055 (S1555), AZD2014 (S2783) and BEZ235 (S1009). Stock solutions were prepared in dimethylsulfoxide (DMSO) and stored at -20°C.
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3

Comprehensive Cell Line Evaluation with EGFR-TKIs

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Human AML cell lines THP-1, U937, KG-1, and HL60 were obtained from the Korean Cell Line Bank (Seoul National University, Seoul, Korea), and the lung cancer cell line A549 was obtained from American Type Culture Collection (ATCC, Manassas, VA, USA). All cells were maintained in RPMI-1640 medium (HyClone; GE Healthcare Life Sciences, Logan, UT, USA) supplemented with 10% fetal bovine serum (FBS; Gibco, Thermo Fisher Scientific, Grand Island, NY, USA) and penicillin–streptomycin. The EGFR-TKIs afatinib, erlotinib, gefitinib, lapatinib, and pelitinib were obtained from Selleck Chemicals. Stock solutions of all drugs were prepared in dimethyl sulfoxide (DMSO; Sigma-Aldrich, St. Louis, MO, USA) and stored at − 80 °C.
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