Table 1.

Antiproliferative activity of EGFR inhibitors in chordoma cell lines

IC50 (μmol/L; in brackets StdDev)
Cell lineU-CH1UM-Chor1MUG-Chor1U-CH2 (Ch. F.)U-CH2 (ATCC)Chor-IN-1JHC7A431 ctrlA2780 ctrl
A. Approved EGFR inhibitors
Afatinib0.0140.0230.2580.4940.5310.6681.3460.0261.915
(0.005)(0.007)(0.072)(0.409)(0.203)(0.351)(0.394)(0.009)(0.594)
Erlotinib0.1440.6173.0068.0427.7762.3292.2810.3463.919
(0.049)(0.069)(0.977)(1.714)(1.953)(0.774)(0.848)(0.033)(0.898)
Lapatinib0.6560.516>10>10>10>10>100.5623.578
(0.257)(0.080)(—)(—)(—)(—)(—)(0.061)(0.771)
Gefitinib0.7910.7516.2416.2595.9369.0407.0100.3334.762
(0.446)(0.055)(1.390)(2.502)(2.115)(1.389)(0.856)(0.069)(0.911)
B. Other advanced EGFR inhibitors
Neratinib0.0380.1101.9461.9263.2532.0092.8930.2820.603
(0.031)(0.023)(0.233)(0.189)(0.470)(0.569)(0.505)(0.059)(0.132)
Dacomitinib<0.019<0.0192.0752.4002.1450.4181.2300.0432.715
(—)(—)(0.191)(0.042)(0.276)(0.054)(0.156)(0.014)(0.106)
Osimertinib0.4590.5691.1292.2501.1650.3840.8970.6463.655
(T790M)(0.120)(0.034)(0.228)(0.085)(0.134)(0.021)(0.113)(0.199)(0.049)
Rociletinib2.1242.1083.6233.6313.6881.9733.2361.5991.026
(T790M)(0.484)(0.586)(1.520)(1.152)(0.684)(1.250)(0.683)(1.527)(0.152)
Doxorubicin0.1660.0670.4550.1520.3480.3400.8810.0830.010
(0.043)(0.040)(0.185)(0.038)(0.191)(0.119)(0.164)(0.004)(0.005)
  • NOTE: In bold, registered EGFR inhibitors. The average IC50 (μmol/L) were determined as described under the Materials and Methods.

  • All values were derived from technical duplicates and confirmed in multiple (n > 6) independent biological experiments.

  • A431 and A2780 cell lines are shown for comparison. Doxorubicin is used as reference standard.