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Table 1 IC50 of various EGFR-TKIs in the transfectant Ba/F3 cell lines

From: Efficacy of irreversible EGFR-TKIs for the uncommon secondary resistant EGFR mutations L747S, D761Y, and T854A

EGFR-TKI

IC50 (nM)

L858R

L858R/L747S

L858R/D761Y

L858R/T854A

L858R/T790 M

First-generation

gefitinib

3.38 (1)

15.1 (5.6)

29.4 (8.7)

222 (68)

8568 (2535)

erlotinib

1.82 (1)

8.68 (4.8)

11.1 (6.2)

85.9 (47)

5377 (2955)

Second-generation

afatinib

0.21 (1)

0.24 (1.1)

0.82 (3.9)

2.13 (10)

73.1 (116)

dacomitinib

0.27 (1)

0.41 (1.5)

1.16 (4.3)

3.19 (12)

38.1 (146)

neratinib

6.44 (1)

13.91 (2.2)

23.8 (3.7)

77.2 (12)

707 (110)

Third-generation

osimertinib

1.98 (1)

1.74 (0.9)

2.74 (1.4)

1.98 (1)

3.67 (1.3)

rociletinib

5.22 (1)

4.69 (0.9)

6.71 (1.3)

6.94 (1.3)

7.08 (1.4)

  1. IC 50 50% inhibitory concentration, EGFR-TKI epidermal growth factor receptor tyrosine kinase inhibitor
  2. The numbers in parentheses indicate the percentages of the actual IC50 value for each mutant relative to that of L858R